solo para uso en investigación

Dexamethasone Agonista del Glucocorticoid Receptor

Name: Dexamethasone
Brand: Selleck Chemicals
SKU: S1322
Rating: 5 (129 reviews)

Cat. No.S1322

La Dexamethasone es un potente miembro sintético de la clase de fármacos esteroides glucocorticoides, y un modulador del receptor de interleucinas que tiene efectos antiinflamatorios e inmunosupresores. La Dexamethasone induce la autophagy y la mitophagy. La Dexamethasone se prueba en pacientes hospitalizados con COVID-19 y se encuentra que tiene beneficios para pacientes críticamente enfermos.

Dexamethasone IL Receptor modulador Chemical Structure

Estructura química

Peso molecular: 392.46

Saltar a

Control de calidad

Lote: Pureza: 99.68%

99.68

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	PMID
human monocytes	Function assay	5 μM	20 h	Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced COX2 expression at 5 uM after 20 hrs using rabbit polyclonal antibody IgG by SDS-PAGE analysis	21843935
rat polymorphonuclear leukocytes	Function assay		20 mins	Antiinflammatory activity in rat polymorphonuclear leukocytes assessed as inhibition of LPS-stimulated nitric oxide production after 20 mins by Griess method, IC50=2.3 nM	22506620
mouse thymocytes	Function assay	1 μM	24 h	Induction of apoptosis in mouse thymocytes assessed as internucleosomal DNA fragmentation at 1 uM after 24 hrs by agarose gel electrophoresis	24794748
T-cell	Function assay			Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells, IC50 = 0.005 μM.	11229767
PBMC	Function assay			Inhibitory concentration against TNF-alpha production from human peripheral blood mononuclear cells stimulated by LPS, IC50 = 0.01 μM.	11229767
PBMC	Function assay			Inhibitory concentration against growth of LPS stimulated human peripheral blood mononuclear cells, IC50 = 0.04 μM.	11229767
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as effect on TNFalpha formation pretreated 1 hr before LPS challenge measured after 24 hrs, IC50 = 0.7 μM.	11908984
N9	Function assay			Inhibitory activity against TNF-alpha release in N9 cells in the supernatant, IC50 = 0.074 μM.	12361395
RAW 264.7	Function assay			Inhibitory activity against TNF-alpha release in RAW 264.7 cells in the supernatant, IC50 = 0.42 μM.	12361395
A549	Function assay	10 uM		Antagonist activity for Glucocorticoid receptor in MMTV transactivation assay in human A549 lung epithelial cells at 10 uM, IC50 = 10 μM.	15999989
A549	Function assay			Activity at glucocorticoid receptor in human A549 cells assessed as effect on GRE promoter response by luciferase reporter assay, EC50 = 0.001 μM.	16643060
A549	Function assay			Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to Dexamethasone, EC50 = 0.005012 μM.	16821781
A549	Function assay			Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells, IC50 = 0.001175 μM.	16821781
HFF	Function assay			Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay, EC50 = 0.0019 μM.	17181172
HeLa	Function assay			Activation of MMTV in HeLa cells measured by luciferase activity, EC50 = 0.017 μM.	17181172
HFF	Function assay			Inhibition of IL1-stimulated IL6 production in HFF cells, IC50 = 0.00051 μM.	17181172
RAW 264.7	Function assay		24 hrs	Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs, IC50 = 0.02 μM.	17367124
RAW264.7	Function assay		2 hrs	Inhibition of COX2 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis	17407277
RAW264.7	Function assay		2 hrs	Inhibition of mPGES1 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis	17407277
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.00537 μM.	17616395
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM.	17616395
A549	Function assay			Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation, IC50 = 1 μM.	17616395
HFF	Antiinflammatory assay			Antiinflammatory activity assessed as inhibition of IL1 stimulated IL6 production in HFF cells by transrepression assay, EC50 = 0.0005 μM.	17692519
HFF	Antiinflammatory assay			Antiinflammatory activity assessed as upregulation of aromatase in HFF cells by transactivation assay, EC50 = 0.002 μM.	17692519
CV1	Function assay			Agonist activity at human GR expressed in CV1 cells by GRE activation assay, EC50 = 0.0002 μM.	17705362
NHDFneo	Function assay			Activity at human GR expressed in NHDFneo cells assessed as inhibition of IL-6 production, IC50 = 0.0014 μM.	17705362
RPMI8226	Antiproliferative assay		4 days	Antiproliferative activity against human RPMI8226 cells after 4 days, IC50 = 0.0065 μM.	17705362
J774A.1	Function assay			Inhibition of LPS-induced TNFalpha production in mouse J774A.1 cells, IC50 = 0.048 μM.	17892941
CV1	Function assay			Activity at human glucocorticoid receptor expressed in CV1 cells assessed as repression of TNF and IL-1-beta-induced E-selectin gene expression by luciferase reporter gene assay, ED50 = 0.0001 μM.	18032610
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.005012 μM.	18038970
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001175 μM.	18038970
COS7	Function assay	1 uM		Agonist activity at glucocorticoid receptor Q570A mutant in COS7 cells at 1 uM by NF-kappaB-luciferase reporter gene assay	18038970
HeLa	Cytotoxicity assay			Cytotoxicity against human HeLa cells assessed as inhibition of DNA replication by imaging analysis	18066055
HeLa	Function assay			Inhibition of mitosis in human HeLa cells by imaging analysis	18066055
R1	Function assay	10 uM	24 hrs	Inhibition of glucocorticoid receptor-glucocorticoid complex transfected in rat R1 cells assessed as down-regulation of TPA-responsive element proinflammatory gene expression at 10 uM after 24 hrs by beta-galactosidase assay, IC50 = 0.005 μM.	18412397
THP1	Antiinflammatory assay			Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 by ELISA, IC50 = 0.007 μM.	18625560
THP1	Antiinflammatory assay			Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha by ELISA, IC50 = 0.05 μM.	18625560
RAW264.7	Function assay	10 uM		Inhibition of LPS-stimulated COX2 expression in mouse RAW264.7 cells at 10 uM by Western blot	18790649
RAW264.7	Function assay			Inhibition of LPS-stimulated microsomal prostaglandin E synthase 1 expression at 10 uM in mouse RAW264.7 cells by Western blot	18790649
A549	Function assay			Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM.	19321341
A549	Function assay			Transrepression activity at GR in PMA-stimulated human A549 cells assessed as inhibition of AP1 response element-induced luciferase reporter gene activity, EC50 = 0.0025 μM.	19321341
NP1	Function assay			Agonist activity at GR ligand binding domain expressed in human NP1 cells assessed as glucocorticoid response element transactivation by GAL4 luciferase reporter gene assay, EC50 = 0.0042 μM.	19321341
TH2	Function assay		48 hrs	Inhibition of pro-inflammatory cytokine IL5 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM.	19323483
TH2	Function assay		48 hrs	Inhibition of pro-inflammatory cytokine IL13 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM.	19323483
MDA-kb2	Function assay			Agonist activity at androgen receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM.	19592245
MDA-kb2	Function assay			Agonist activity at glucocorticoid receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM.	19592245
A549	Function assay			Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM.	19592247
COS7	Function assay			Agonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay, EC50 = 0.0072 μM.	19863083
A549	Function assay		6 hrs	Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of IL-1-beta-induced NF-kappaB dependent E-selection promoter activation after 6 hrs by luciferase reporter gene based ELAM assay, EC50 = 0.0011 μM.	20047280
A549	Function assay		6 hrs	Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of PMA-induced AP1 activity after 6 hrs by luciferase reporter gene assay, EC50 = 0.0025 μM.	20047280
HeLa	Function assay			Transactivation of GAL-4 tagged glucocorticoid receptor ligand binding domain expressed in human HeLa cells assessed as NP1 activation by luciferase reporter gene assay, EC50 = 0.0045 μM.	20047280
NIH-3T3	Function assay	0.01 mg/kg	1 hr	Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Cp = 0.044 μM.	20469868
NIH-3T3	Function assay	0.1 mg/kg	1 hr	Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Cp = 0.236 μM.	20469868
NIH-3T3	Function assay	1 mg/kg	1 hr	Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Cp = 1.8 μM.	20469868
NIH-3T3	Function assay	10 mg/kg	1 hr	Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Cp = 17.7 μM.	20469868
NIH-3T3	Function assay	0.01 mg/kg	1 hr	Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Fu = 0.00203 μM.	20469868
NIH-3T3	Function assay	0.1 mg/kg	1 hr	Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Fu = 0.0116 μM.	20469868
NIH-3T3	Function assay	1 mg/kg	1 hr	Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Fu = 0.087 μM.	20469868
NIH-3T3	Function assay	10 mg/kg	1 hr	Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Fu = 5.123 μM.	20469868
HeLa	Function assay			Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, EC50 = 0.007943 μM.	20727743
HeLa	Function assay			Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay, IC50 = 0.001585 μM.	20727743
THP1	Function assay			Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8 production, IC50 = 0.002512 μM.	20727743
Sf9	Function assay			Binding affinity to human recombinant glucocorticoid receptor expressed in baculovirus infected Sf9 cells, IC50 = 0.01259 μM.	20727743
insect cells	Function assay			Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.0034 μM.	20735001
insect cells	Function assay			Binding affinity to mineralocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.033 μM.	20735001
U2OS	Function assay		18 hrs	Agonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay, EC50 = 15.8489 μM.	20812681
U2OS	Function assay		18 hrs	Antagonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay, IC50 = 0.0005082 μM.	20812681
HepG2	Function assay		24 hrs	Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis, EC50 = 2.6 μM.	20966043
A549	Function assay			Transrepression activity of glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM.	21073190
A549	Function assay			Transrepression activity of glucocorticoid receptor in human A549 cells expressing AP-1 assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay, EC50 = 0.0025 μM.	21073190
NP-1 Hela	Function assay			Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay, EC50 = 0.0042 μM.	21073190
13D3/Huh7	Function assay		24 hrs	Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs, EC50 = 0.005 μM.	21073190
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM.	21257309
A549	Function assay			Agonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, IC50 = 0.003981 μM.	21257309
RAW264.7	Antiinflammatory assay		18 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 2 hrs before LPS challenge measured after 18 hrs by griess reaction, IC50 = 0.86 μM.	21288727
HMC1	Function assay		1 hr	Immunomodulatory activity in human HMC1 cells assessed as inhibition of phorbol 12-myristate 13-acetate/A23187-stimulated IL1-beta secretion treated 1 hr prior to 30 mins phorbol 12-myristate 13-acetate/A23187 challenge by Western blotting analysis	21302967
RAW264.7	Antiinflammatory assay	10 uM	24 hrs	Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as nitrite level at 10 uM after 24 hrs by Griess method, Activity = 1.54 μM.	21353543
RAW264.7	Antiinflammatory assay		18 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs, IC50 = 0.01 μM.	21353543
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method, IC50 = 0.8 μM.	21353543
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction, IC50 = 0.02 μM.	21361338
RAW264.7	Function assay		20 mins	Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells pre-incubated for 20 mins before LPS challenge measured 18 hrs post LPS challenge by Griess method	21775152
RAW264.7	Function assay		30 mins	Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells pre-incubated for 30 mins before LPS challenge measured 6 hrs post LPS challenge by ELISA	21775152
HeLa	Function assay			Agonist activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, EC50 = 0.017 μM.	21963986
insect cells	Function assay			Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.003 μM.	21963986
insect cells	Function assay			Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.033 μM.	21963986
RAW264.7	Antiinflammatory assay		2 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method, IC50 = 0.47 μM.	22372956
RAW264.7	Antiinflammatory assay		2 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method, IC50 = 0.98 μM.	22537362
A549	Antiinflammatory assay	1 uM	30 mins	Antiinflammatory activity in human A549 cells assessed as inhibition of IL-1beta-induced mPGES1 expression at 1 uM treated 30 mins prior to IL-1beta challenge measured after 48 hrs by Western blot analysis relative to control	22795900
H13	Function assay		3 hrs	Inhibition of glucocorticoid receptor in human H13 cells assessed as inhibition of glucocorticoid-induced cell proliferation after 3 hrs by [3H]-thymidine incorporation assay, EC50 = 0.0097 μM.	23199485
293 MSR	Function assay		60 mins	Displacement of [3H]-dexamethasone human glucocorticoid receptor alpha expressed in 293 MSR cells after 60 mins by scintillation counting, EC50 = 0.0125 μM.	23199485
IOBA-NHC	Function assay	40 uM	24 hrs	Inhibition of NF-kappaB p65-mediated IL-6 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA	23219855
IOBA-NHC	Function assay	40 uM	24 hrs	Inhibition of NF-kappaB p65-mediated TNFalpha release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA	23219855
IOBA-NHC	Function assay	40 uM	24 hrs	Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA	23219855
HCLE	Function assay	40 uM	24 hrs	Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human HCLE cells at 40 uM after 24 hrs by ELISA	23219855
HCT116	Function assay	20 to 40 uM	24 hrs	Agonist activity at glucocorticoid receptor (unknown origin) expressed in human HCT116 cells co-expressing GRE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay	23276449
RAW264.7	Antiinflammatory assay		2 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 2 hrs prior to LPS-challenge measured after 24 hrs by Griess method, IC50 = 1.43 μM.	23373965
HeLaS3	Function assay		2 hrs	Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, IC50 = 0.0041 μM.	23403082
HeLaS3	Function assay		2 hrs	Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, Ki = 0.0022 μM.	23403082
A549	Function assay			Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM.	23916594
A549	Function assay			Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-stimulated AP1 response element by luciferase reporter gene assay, EC50 = 0.0025 μM.	23916594
Hela	Function assay			Transactivation activity at glucocorticoid receptor ligand binding domain (unknown origin) expressed in human Hela cells co-expressing GAL4 DNA binding domain assessed as NP-1-stimulated GRE activation by luciferase reporter gene assay, EC50 = 0.0045 μM.	23916594
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL-1beta-induced NF-kappaB dependent E-selectin activation by luciferase reporter gene assay, EC50 = 0.0011 μM.	23953070
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activation by luciferase reporter gene assay, EC50 = 0.0025 μM.	23953070
HeLa	Function assay			Transactivation of glucocorticoid receptor ligand binding domain (unknown origin) transfected in human HeLa cells assessed as activation of NP-1 by GAL4 luciferase reporter gene assay, EC50 = 0.0045 μM.	23953070
A549	Function assay			Transrepression of glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay, EC50 = 0.0025 μM.	24011644
HeLa	Function assay			Transactivation of GR-LBD expressed in human HeLa cells co-expressing GAL4-DBD by luciferase reporter gene assay, EC50 = 0.0042 μM.	24011644
HEK293	Function assay			Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells, Ki = 0.00036 μM.	24446728
HEK293	Function assay			Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells, Ki = 0.00069 μM.	24446728
HEK293	Function assay			Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells, Ki = 0.561 μM.	24446728
HEK293	Function assay			Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells, Ki = 1.41 μM.	24446728
HeLa	Function assay			Transactivation of glucocorticoid receptor in human HeLa cells harboring MMTV promoter by luciferase reporter gene assay, EC50 = 0.017 μM.	24656565
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells assessed as E-selectin transrepression by luciferase reporter gene assay, EC50 = 0.0011 μM.	24980053
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells assessed as AP-1 transrepression by luciferase reporter gene assay, EC50 = 0.0025 μM.	24980053
HeLa	Function assay			Agonist activity at glucocorticoid receptor in human HeLa cells assessed as NP-1 transactivation by luciferase reporter gene assay, EC50 = 0.0045 μM.	24980053
B16F10	Antitumor assay	20 mg/kg	24 days	Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as inhibition tumor growth at 20 mg/kg, ip measured after 24 days of tumor inoculation	24992071
B16F10	Antitumor assay	20 mg/kg	24 days	Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by TUNEL assay	24992071
B16F10	Apoptosis assay	10 uM	48 hrs	Induction of apoptosis in mouse B16F10 cells assessed as increase in ratio of BAX/Bcl2 expression at 10 uM after 48 hrs by Western blot analysis relative to untreated control	24992071
B16F10	Antitumor assay	20 mg/kg	24 days	Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by VE-cadherin	24992071
CUTLL1	Growth inhibition assay		48 hrs	Growth inhibition of human CUTLL1 cells with high GR expression levels after 48 hrs by alamar blue assay	25050160
HEK293	Function assay			Agonist activity at human GCR expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.0013 μM.	25305688
RAW264.7	Function assay		24 hrs	Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay relative to vehicle-treated control, IC50 = 0.8 μM.	25499882
HFF	Function assay			Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production, IC50 = 0.001 μM.	25516791
RAW264.7	Antiinflammatory assay	1 mM	30 mins	Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction of LPS-induced TNF mRNA expression cells at 1 mM treated 30 mins before LPS challenge measured after 3 hrs by qRT-PCR analysis	25667960
SW1353	Function assay		24 hrs	Transrepression activity at glucocorticoid receptor in human SW1353 cells assessed as repression of IL-1-induced MMP-13 production after 24 hrs by ELISA, IC50 = 0.0018 μM.	25706100
RAW264.7	Function assay		6 hrs	Inhibition of TNFalpha production in mouse RAW264.7 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.04 μM.	25824662
J774A.1	Function assay		6 hrs	Inhibition of TNFalpha production in mouse J774A.1 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.4 μM.	25824662
RAW264.7	Function assay		12 hrs	Inhibition of IL-1beta production in mouse RAW264.7 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 4.7 μM.	25824662
J774A.1	Function assay		12 hrs	Inhibition of IL-1beta production in mouse J774A.1 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 22 μM.	25824662
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.63 μM.	26087384
BV2	Antiinflammatory assay		24 hrs	Antiinflammatory activity in C57BL6/J mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.025 μM.	26110443
RAW264.7	Function assay		24 hrs	Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 0.8 μM.	26305406
J774	Antiinflammatory assay	10 uM	24 hrs	Antiinflammatory activity against mouse J774 cells assessed as inhibition of LPS-induced iNOS expression at 10 uM after 24 hrs by Western blot analysis	26915998
IM9	Function assay			Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cells, IC50 = 0.0038 μM.	26988801
C57BL/6	Antiinflammatory assay	10 mg/kg	1 hr	Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced mononuclear cells migration in articular cavity at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs	27227459
C57BL/6	Antiinflammatory assay	10 mg/kg	1 hr	Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced infiltration of inflammatory cells into synovial tissue at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs by hematoxylin and eosin stai	27227459
J774A.1	Antiinflammatory assay	1 uM	1 hr	Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced IL6 production in cell-free supernatant at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by sandwich ELISA	27227459
J774A.1	Antiinflammatory assay	1 uM	1 hr	Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced COX2 expression at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by Western blot analysis	27227459
J774A.1	Antiinflammatory assay	1 uM	1 hr	Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced nitric oxide production at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by colorimetric Griess test	27227459
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs in presence of LPS by Griess assay, IC50 = 0.63 μM.	27825545
IM9	Function assay			Displacement of [3H]dexamethasone from GR receptor in human IM9 cells, IC50 = 0.0038 μM.	27876250
HeLa	Function assay			Transrepression activity at glucocorticoid receptorin human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay, IC50 = 0.001585 μM.	28043796
THP1	Function assay			Transrepression activity at glucocorticoid receptor in human THP1 cells assessed as receptor-mediated anti-inflammatory activity by measuring inhibition of LPS-induced IL-8 production, IC50 = 0.002512 μM.	28043796
HeLa	Function assay			Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, IC50 = 0.007943 μM.	28043796
Sf9	Function assay			Binding affinity to recombinant human glucocorticoid receptor expressed in baculovirus infected sf9 cells, IC50 = 0.01259 μM.	28043796
RAW264.7	Antiinflammatory assay		30 mins	Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production pretreated for 30 mins followed by LPS stimulation for 24 hrs by Griess assay, IC50 = 7 μM.	28499733
RAW264.7	Function assay		24 hrs	Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 2.5 μM.	28598633
Mino	Antiproliferative assay	100 uM	48 hrs	Antiproliferative activity against human Mino cells at 100 uM preincubated for 48 hrs followed by thymidine addition measure after 16 hrs by Thymidine incorporation assay	28858511
RAW264.7	Antiinflammatory assay			Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by griess assay, IC50 = 0.8 μM.	29272126
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in COX2 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in NO production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by Grie	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs b	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by EL	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 3 hrs by	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS protein level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by	29389121
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BV2	Antiinflammatory assay			Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production, IC50 = 9.5 μM.	29482940
RAW264.7	Function assay		24 hrs	Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 10.7 μM.	29518326
HeLa	Function assay	0.4 uM	24 hrs	Transrepression of GCR in human HeLa cells assessed as suppression of DEX-induced GILZ mRNA expression at 0.4 uM after 24 hrs by Taqman-based real-time PCR analysis	29670697
RAW264.7	Antiinflammatory assay			Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production, IC50 = 8.3 μM.	29741372
HEK 293T	Function assay			Agonist activity at GAL4 DNA-binding domain fused GR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay, IC50 = 0.00235 μM.	30144697
RAW264.7	Antiinflammatory assay	20 uM	6 hrs	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA	30215255
RAW264.7	Antiinflammatory assay	20 uM	6 hrs	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-1beta production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA	30215255
RAW264.7	Antiinflammatory assay	20 uM	6 hrs	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA	30215255
RAW264.7	Antiinflammatory assay	20 uM	6 hrs	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA	30215255
Haga clic para ver más datos experimentales de líneas celulares

Información química, almacenamiento y estabilidad

Peso molecular	392.46	Fórmula	C₂₂H₂₉FO₅	Almacenamiento (Desde la fecha de recepción)	2 years 4°C, in dark and seal
Nº CAS	50-02-2	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	NSC 34521, Hexadecadrol, Prednisolone F,MK-125			Smiles	CC1CC2C3CCC4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)CO)O)C)O)F)C

Solubilidad

In vitro
Lote:

DMSO : 78 mg/mL (198.74 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 11 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	1.350mg/ml (3.44mM)	Taking the 1 mL working solution as an example, add 50 μL of 27 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	1% DMSO 1 40% PEG300 2 5% Tween 3 54%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	0.375mg/ml (0.96mM)	Taking the 1 mL working solution as an example, add 10 μL of 37.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 540 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción

Targets/IC₅₀/Ki	interleukin receptor (Cell-free assay)
In vitro	La Dexamethasone provoca una disminución de la permeabilidad paracelular transmonocapa principalmente a la sacarosa, la fluoresceína y los dextranos de hasta 20 KDa en una línea celular endotelial de cerebro de rata inmortalizada (GPNT). Este compuesto hace que la actina filamentosa y la proteína cortactina asociada al citoesqueleto se concentren altamente en las regiones de contacto célula-célula con pocas fibras de estrés de actina F visibles dentro del citoplasma en células endoteliales de cerebro de rata cultivadas, una observación consistente con un fenotipo de barrera más diferenciado inducido por esta sustancia química. Se ha demostrado que su tratamiento estimula fuertemente el nivel de la proteína Id-1, que es un represor transcripcional hélice-bucle-hélice inducible por suero, involucrado en la diferenciación celular, y se demostró que este efecto se asocia con la reorganización de ZO-1 a la periferia celular en células tumorales epiteliales mamarias Con8. Previene el aumento de la expresión de MMP-9 inducida por citoquinas y las alteraciones en la expresión de ZO-1 en monocapas de GPNT no tratadas. Este compuesto agota los niveles basales y los estimulados por TNF-alfa de GSH al regular a la baja la transcripción de la subunidad pesada de gamma-GCS a través de un mecanismo que involucra a AP-1 (c-Jun) en las células epiteliales alveolares. Disminuye los niveles de GSH basales y estimulados (tratados con TNF-α) en las células epiteliales alveolares (A549), sin ningún cambio en el GSSG.
In vivo	La Dexamethasone se administra i.m. a ovejas preñadas, lo que da lugar a los siguientes resultados: (1) la presión arterial no cambia; (2) como se informó previamente en el feto, la sensibilidad a la endotelina-1 (ET) aumenta; (3) la relajación inducida por acetilcolina aumenta; (4) la respuesta vasodilatadora a la ET suprimible por L-NAME se anula; (5) no hay cambios en la vasodilatación independiente del endotelio; y (6) no hay cambios en los niveles de ARN y proteína de eNOS, en comparación con los controles tratados con solución salina.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/12782340/ [2] https://pubmed.ncbi.nlm.nih.gov/11007940/ [3] https://pubmed.ncbi.nlm.nih.gov/12562957/ [4] https://pubmed.ncbi.nlm.nih.gov/16166452/ [5] https://pubmed.ncbi.nlm.nih.gov/17440100/ [6] https://pubmed.ncbi.nlm.nih.gov/28263313/ [7] https://pubmed.ncbi.nlm.nih.gov/35544603/

Aplicaciones

Métodos	Biomarcadores	Imágenes	PMID
Western blot	Bcl-2 / Bcl-xl / Mcl-1 / Survivin / IAP1 Cyclin D1 / Cyclin E / COX-2 / MMP-9 Bax / p21 p-JNK / JNK / p-p38 / p38 / p-ERK / ERK		28696369

Información del ensayo clínico

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT06351644	Not yet recruiting	Relapsed and/or Refractory Multiple Myeloma	Adriana Rossi\|Icahn School of Medicine at Mount Sinai	June 3 2024	Phase 1\|Phase 2
NCT06367855	Not yet recruiting	Spinal Stenosis Lumbar\|Disc Degeneration\|Disc Disease\|Fusion of Spine\|Surgery	Potsawat Surabotsopon\|Thammasat University Hospital	May 1 2024	Phase 4
NCT06367725	Recruiting	Acute Lymphoblastic Leukemia	University of Aarhus	April 11 2024	--

Soporte técnico

Instrucciones de manipulación

Tel: +1-832-582-8158 Ext:3

Si tiene alguna otra consulta, por favor deje un mensaje.

Preguntas frecuentes

Pregunta 1:
I'm looking for it to use in cell culture. Would it be better to use the S1322, the sodium phosphate S4028, or the acetate S3124?

Respuesta:
S1322 is the free base form of this compound, S4028 is the sodium phosphate form and S3124 is the acetate salt. All of them have similar biological activity in tissue culture, however, their suitabilities vary in different solvents. As free base, S1322 has high solubility in DMSO (79mg/ml), poor solubility in water (<1mg/ml), and moderate solubility in ethanol (6mg/ml). As sodium phosphate salt, S4028 has high solubility in water (103mg/ml) but is insoluble in DMSO and ethanol (<1mg/ml). The solubility of S3124 is 87mg/ml in DMSO, <1mg/ml in water, and 20mg/ml in ethanol. Selection can be made based on the customer's experimental setup.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):