Home Immunology & Inflammation Antineoplastic and Immunosuppressive Antibiotics inhibidor Cyclosporin A

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Cyclosporin A inhibidor de Calcineurin

Cat. No.S2286

Cyclosporin A, un oligopéptido cíclico no polar, es un agente inmunosupresor que se une a la ciclofilina y luego inhibe la calcineurina con una IC50 de 7 nM en un ensayo sin células. La Cyclosporin A se administra generalmente después de una cirugía de trasplante para prevenir el rechazo y se ha utilizado para probar su efecto tóxico en un modelo de túbulo proximal 3D perfundido. Cyclosporin A (NSC 290193) se puede usar para inducir modelos animales de rechazo crónico de trasplante de hígado.
Cyclosporin A Antineoplastic and Immunosuppressive Antibiotics inhibidor Chemical Structure

Estructura química

Peso molecular: 1202.61

Saltar a

Control de calidad

Lote: Pureza: 99.98%
99.98

Productos que se suelen utilizar junto con Cyclosporin A

Diquafosol Tetrasodium

Combination therapy with it and Diquafosol Tetrasodium significantly improves the objective signs and symptoms of dry eyes.

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad PMID
rat H42E cells Cytotoxic assay Cytotoxicity against rat H42E cells assessed as intracellular ATP level, TC50=42 μM 19502058
mouse L929 cells Cytotoxic assay 3 days Cytotoxicity against mouse L929 cells after 3 days by MTS assay, IC50=30 μM 25985195
human Huh-Mono cells Cytotoxic assay 3 days Cytotoxicity against human Huh-Mono cells after 3 days by MTT assay， CC50=24 μM 18625766
MDCK cells Cytotoxic assay Cytotoxicity against MDCK cells, TC50=9.9 μM 18212100
human LCC-6 cells Cytotoxic assay 72 h Cytotoxicity against human LCC-6 cells after 72 hrs, IC50=8.3 μM 22320402
human HeLa cells Cytotoxic assay Cytotoxicity against human HeLa cells, TC50=8.3 μM 18212100
african green monkey Vero cells Function assay 24 h Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay, IC50=8 μM 19451286
human Huh-9-13 cells Cytotoxic assay 3 days Cytotoxicity against human Huh-9-13 cells after 3 days by MTT assay， CC50=7 μM 18625766
human HuH6 cells Cytotoxic assay 3 days Cytotoxicity against human HuH6 cells after 3 days by MTT assay, CC50=7 μM 18625766
human Huh5-2 cells Cytotoxic assay 3 days Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay , CC50=6 μM 18625766
human HuH7 cells Cytotoxic assay Cytotoxicity against human HuH7 cells assessed as release of lactate dehydrogenase, IC50=5.81 μM 20943390
human 2008 cells Function assay Inhibition of human MRP1 in human 2008 cells, IC50=4.78 μM 18707884
human HeLa cells Function assay Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 7 days， TC50=4.6 μM 18212100
leukemia CEM cells Function assay Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells, IC50=3.4 μM 12361387
human Caco2 cells Function assay nhibition of P-gp in human Caco2 cells assessed as reduction in digoxin efflux, IC50=2.9 μM 23382458
human MDA435/LCC6MDR cells Cytotoxic assay 72h Cytotoxicity against human MDA435/LCC6MDR cells expressing MDR after 72 hrs， IC50=2.8 μM 22320402
guinea pig ventricular myocytes Function assay Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes, IC50=2 μM 22761000
KB/MDR cell Function assay 72 h Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure, IC50=1.5 μM 15481991
A2780/ADR cells Function assay Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay， IC50=1.41254 μM 17890094
human K562/R7 cells Function assay 1 μM 72 h Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay, IC50=0.7 μM 25634041
LLC-PK1 epithelial cells Function assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay， IC50=0.7 μM 12699389
mouse L5178 cells Function assay 20 mins Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 after 20 mins by FACS analysis, IC50=0.65 μM 21341745
KB cell Function assay Inhibitory activity against KB cell line after 72 h of drug exposure, IC50=0.6 μM 15481991
mouse mammary carcinoma cell line EMT6/AR 1.0 Function assay Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.0, IC50=0.44 μM 10098671
CK1 cells Function assay Antiviral activity against HPV-33 infected in CK1 cells assessed as inhibition of viral replication after 7 days, TC50=0.3 μM 18212100
HEK293 cells Function assay Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as protein-mediated pitavastatin uptake， Ki=0.2 μM 22587986
human MDA435/LCC6MDR cells Function assay 5 days Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing paclitaxel resistance measured as cell survival after 5 days by MTS assay, EC50=0.032 μM. 25985195
human PBMC Proliferation assay Antiproliferative activity against human PBMC, IC50=12 nM 15679309
mouse T cells Function assay 4 days Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay, ic50=11 nM 22984987
human splenocytes Function assay 4 days Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay, IC50=10 nM 19827831
human T-cell Function assay In vitro inhibitory activity against human T-cell production of lymphokine IL-2, IC50=8.1 nM 7537331
human Jurkat cells Function assay 1 h Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay, EC50=5 nM 19933795
human PBMC Function assay 1 h Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay, EC50=3.1 nM 19933795
Jurkat cells Function assay Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells, IC50=2 nM 14643337
HepG2 cells Function assay Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50=1.65 nM 22586124
Jurkat Function assay The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells., IC50 = 0.012 μM. 7473543
mouse spleen cells Function assay The compound was tested in vitro for inhibition of proliferation in BDF1 mouse spleen cells stimulated with concanavalin A (ConA)., IC50 = 0.04 μM. 7473543
Sf9 Function assay inhibition of Verapamil stimulated ATP hydrolysis in membranes from MDR1-expressing Sf9 cells, Ki = 0.02 μM. 7514263
LLC-PK1 Function assay transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells, Km = 8.4 μM. 7681059
HeLa Function assay inhibition of LTC4 uptake in membrane vesicle from MRP1-expressing HeLa cells, Ki = 5 μM. 7961706
Caco-2 Function assay transepithelial transport (basal to apical) in Caco-2 cells, Km = 3.8 μM. 8842452
spleen Function assay Effect of compound on IL-2 production from alloantigen-stimulated mouse spleen cells, IC50 = 0.01 μM. 8893839
COS Function assay inhibition of Taurocholate uptake in ASBT-expressing COS cells, Ki = 24 μM. 9458785
LLC-PK1 Function assay inhibition of Doxorubicin transepithelial transport (basal to apical) (Digoxin: 0.8 uM) in MDR1-expressing LLC-PK1 cells, IC50 = 3.66 μM. 9914792
CEM/VLB100 Function assay inhibition of Calcein-AM efflux in CEM/VLB100 cells, Ki = 1.8 μM. 10198227
HEK Function assay inhibition of BMG uptake in membrane vesicles from Mrp2-expressing HEK cells, Ki = 10 μM. 10421658
HEK Function assay inhibition of BMG uptake in membrane vesicles from MRP2-expressing HEK cells, Ki = 21 μM. 10421658
HeLa Function assay inhibition of Taurocholate uptake in NTCP-expressing HeLa cells, IC50 = 1 μM. 10565843
LLC-PK1 Function assay inhibition of LTC4 uptake in membrane vesicles from MRP2-expressing LLC PK1 cells, Ki = 4.7 μM. 10570049
Sf9 Function assay inhibition of Taurocholate uptake in membrane vesicles from Bsep-expressing Sf9 cells, Ki = 0.3 μM. 10648470
Caco-2 Function assay inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells, IC50 = 1.3 μM. 10820137
CEM/VLB100 Function assay inhibition of Calcein-AM efflux (Calcein-AM: 0.25 uM) in CEM/VLB100 cells, IC50 = 3.41 μM. 10891114
Sf9 Function assay inhibition of ATPase in membrane vesicle from BCRP-expressing Sf9 cells, Ki = 0.5 μM. 11437380
NIH-3T3-G185 Function assay inhibition of Daunorubicin efflux in NIH-3T3-G185 cells, IC50 = 1.4 μM. 11716514
NIH-3T3-G185 Function assay inhibition of Calcein-AM efflux in NIH-3T3-G185 cells, IC50 = 1.7 μM. 11716514
NIH-3T3-G185 Function assay inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells, IC50 = 1.7 μM. 11716514
NIH-3T3-G185 Function assay inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50 = 1.8 μM. 11716514
NIH-3T3-G185 Function assay inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells, IC50 = 2.1 μM. 11716514
NIH-3T3-G185 Function assay inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells, IC50 = 2.4 μM. 11716514
NIH-3T3-G185 Function assay inhibition of JC-1 efflux in NIH-3T3-G185 cells, IC50 = 4.3 μM. 11716514
HCT15 Function assay 0.4 to 6.3 ug/mL Modulation of P-gp in human HCT15 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL. 11754602
UO31 Function assay 0.4 to 6.3 ug/mL Modulation of P-gp in human UO31 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL. 11754602
CAKI1 Function assay 0.4 to 6.3 ug/mL Modulation of P-gp in human CAKI1 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL. 11754602
MDA-435/LCC6 and MDA-435/LCC6-MDRI Function assay Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%., EC50 = 0.5 μM. 11784143
MDA-435/LCC6 Function assay Effect on reversal of [3H]- VBL accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50 = 0.6 μM. 11784143
MDA-435/LCC6 and MDA-435/LCC6-MDRI Function assay Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%, EC50 = 0.6 μM. 11784143
MDA435/LCC6 MDR1 Function assay reversal of Vinblastine accumulation (Vinblastine: 0.005 uM) in MDA435/LCC6 MDR1 cells, EC50 = 0.6 μM. 11784143
MDA-435/LCC6 (Pgp-negative) Function assay Effect on reversal of DOX accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50 = 0.7 μM. 11784143
MDA-435/LCC6 Growth inhibitory assay Growth inhibitory activity on MDA-435/LCC6 (Pgp-positive) human breast cancer cells., IC50 = 1 μM. 11784143
MDA-435/LCC6-MDRI Growth inhibitory assay Growth inhibitory activity on MDA-435/LCC6-MDRI (Pgp-negative) human breast cancer cells., IC50 = 1.1 μM. 11784143
BTI-TN5B1-4 Function assay ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells, Km = 0.17 μM. 11785684
Jurkat Function assay Inhibition of production of IL-2 secretion in Jurkat cells, IC50 = 0.007 μM. 11881984
Jurkat Function assay Inhibition of production of beta-galactosidase IL-2 RGA in Jurkat cells, IC50 = 0.008 μM. 11881984
LLC-PK1 Function assay increase in Vinblastine intracellular accumulation in MDR1-expressing LLC-PK1 cells, Ki = 1.3 μM. 11961113
LLC-PK1 Function assay increase in Calcein-AM intracellular accumulation in MDR1-expressing LLC-PK1 cells, Ki = 4.66 μM. 11961113
MDCK Function assay inhibition of Digoxin transepithelial transport (basal to apical) in MDR1-expressing MDCK cells, Ki = 2.18 μM. 12134945
MDCK Function assay inhibition of Vinblastine transepithelial transport (basal to apical) in MRP2-expressing MDCK cells, Ki = 8.11 μM. 12134946
LLC-PK1 Function assay increase in Calcein-AM intracellular accumulation in mdr1b-expressing LLC-PK1 cells, Ki = 3.5 μM. 12235267
LLC-PK1 Function assay increase in Calcein-AM intracellular accumulation in mdr1a-expressing LLC-PK1 cells, Ki = 3.65 μM. 12235267
HL-60 Function assay Inhibitory activity against Human formylpeptide receptor (FPR) of human leukemia HL-60 cells, IC20 = 3.6 μM. 12361388
High Five cells Function assay inhibition of Taurochenodeoxycholate uptake(CsA 30uM, 30 % of control) in membrane vesicles prepared from High Five cells infected with the ABCB11 baculovirus, Ki = 9.5 μM. 12404239
MDCKII Function assay inhibition of Cerivastatin uptake in OATP2-expressing MDCKII cells, Ki = 0.238 μM. 12538813
Caco-2 Function assay transepithelial transport of digoxin (basal to apical) in Caco-2 cells, Ki = 0.35 μM. 12636153
SK-E2 Function assay increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP), IC50 = 7.5 μM. 12739759
SK-E2 Function assay increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP), IC50 = 7.8 μM. 12739759
HEK293 Function assay inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells, Ki = 0.2 μM. 14530907
T-cells Function assay Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method, IC50 = 0.032 μM. 14593182
T-cells Function assay Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method, IC50 = 0.074 μM. 14593182
PMBC Function assay 72 hrs Effect on proliferation of human peripheral blood mononuclear cells (PMBC) at 72 hr using MTT assay, IC50 = 8.97 μM. 15203163
mouse spleen cells Cytotoxicity assay Cytotoxicity against BALB/c mouse spleen cells, CC50 = 1.35 μM. 17081761
MDCK2 Function assay Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells, IC50 = 9.34 μM. 17664327
HEK293 Function assay Inhibition of cross-linking of human Pgp TM1 L65R/TM6 L339C/TM7 F728 mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 0.5 μM. 17848563
HEK293 Function assay Inhibition of cross-linking of human Pgp TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 0.6 μM. 17848563
HEK293 Function assay Inhibition of cross-linking of human Pgp TM3T199R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 1.1 μM. 17848563
HEK293 Function assay Inhibition of cross-linking of human Pgp TM6 F343R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 11 μM. 17848563
HEK293 Function assay Inhibition of cross-linking of human Pgp TM5 I306R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 15 μM. 17848563
MDCK2 Function assay 10 uM 40 mins Inhibition of human wild type Pgp expressed in MDCK2 cells assessed as calcein-AM accumulation at 10 uM after 40 mins. 17964170
A2780 Function assay 30 mins Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay, IC50 = 1.41254 μM. 18083034
A2780 Function assay 30 mins Inhibition of human Pgp in A2780 cells after 30 mins by calcein AM assay, IC50 = 1.41254 μM. 18083034
Caco-2 Function assay Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells, EC50 = 45.5 μM. 18524592
A2780 Function assay Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50 = 1.41254 μM. 18678495
Huh-9-13 Antiviral assay 3 days Antiviral activity against BILN 2061-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.004 μM. 19104013
Huh-9-13 Antiviral assay 3 days Antiviral activity against compound-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.35 μM. 19104013
Huh-9-13 Antiviral assay 3 days Antiviral activity against 2'-C-methyl-2'-fluoro-cytidine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.4 μM. 19104013
Huh-9-13 Antiviral assay 3 days Antiviral activity against VX 950-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.49 μM. 19104013
Huh-9-13 Antiviral assay 3 days Antiviral activity against R479-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 1.98 μM. 19104013
Huh-9-13 Antiviral assay 3 days Antiviral activity against cyclosporine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 3.85 μM. 19104013
A2780/ADR Function assay Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay, IC50 = 1.4 μM. 19250834
C2C12 Function assay 0.1 ug/ml 3 days Inhibition of hexose-6-phosphate dehydrogenase-induced cell differentiation in mouse C2C12 cells assessed as myosin heavy chain fluorescence at 0.1 ug/ml for 3 days. 20081855
C2C12 Function assay Inhibition of serum withdrawal-induced cell differentiation in mouse C2C12 cells assessed as myosin heavy chain expression. 20081855
HuH7 Antiviral assay 48 hrs Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay, EC50 = 0.21 μM. 20176894
HuH7 Antiviral assay 48 hrs Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay, EC50 = 3.39 μM. 20176894
T-cells Immunosuppressive assay 72 hrs Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay, IC50 = 0.06 μM. 21131104
T-cells Cytotoxicity assay 48 hrs Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay, CC50 = 15.82 μM. 21131104
HCT15 Function assay 10 uM Inhibition of MDR1 in human HCT15 cells assessed as calcein-AM efflux at 10 uM by fluorescence assay. 21348461
T-cells Immunosuppressive assay 96 hrs Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay, IC50 = 0.014 μM. 21456524
mouse spleen cells Function assay Inhibition of serine palmitoyltransferase in mouse spleen cells. 21456524
HCT116 Function assay 10 uM 30 mins Modulation of BCRP in human HCT116 cells assessed as intracellular accumulation of mitoxantrone at 10 uM after 30 mins by flow-cytometry. 21488686
Sf21 Function assay Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 0.5 μM. 21965623
Sf21 Function assay Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 0.6 μM. 21965623
T-cells Function assay Inhibition of CD4 expression in human CD4+ T cells, IC50 = 8.97 μM. 22101135
L929 Cytotoxicity assay 72 hrs Cytotoxicity against mouse L929 cells after 72 hrs, IC50 = 33.9 μM. 22320402
CCRF-CEM/VCR1000 Function assay 240 secs Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis, IC50 = 0.10233 μM. 22452412
mouse lymph node cells Immunosuppressive assay 72 hrs Immunosuppressive activity in anti-CD3/anti-CD8 co-stimulated Balb/c mouse lymph node cells assessed as inhibition of cell proliferation after 72 hrs by ELISA, IC50 = 0.07 μM. 22494616
mouse lymph node cells Cytotoxicity assay 48 hrs Cytotoxicity against Balb/c mouse lymph node cells after 48 hrs by MTT assay, CC50 = 10.1 μM. 22494616
HEK293 Function assay 5 mins Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, Ki = 1.2 μM. 22541068
HEK293 Function assay Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, Ki = 1.3 μM. 22541068
HEK293 Function assay 5 mins Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, IC50 = 1.3 μM. 22541068
HEK293 Function assay Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, IC50 = 1.4 μM. 22541068
HEK293 Function assay 5 mins Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, Ki = 36 μM. 22541068
HEK293 Function assay 5 mins Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, IC50 = 37 μM. 22541068
T-cells Immunosuppressive assay 24 hrs Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay, IC50 = 2.12 μM. 22727369
2008 Function assay 10 uM 30 mins Inhibition of human MRP1 expressed in 2008 cells at 10 uM preincubated for 30 mins prior to calcein AM addition measured every 60 secs up to 90 mins by calcein AM accumulation assay. 23017888
A2780adr Function assay 10 uM 30 mins Inhibition of human P-gp overexpressed in doxorubicin resistant A2780adr cells at 10 uM preincubated for 30 mins prior to calcein AM addition measured every 60 secs up to 90 mins by calcein AM accumulation assay. 23017888
HL60 Function assay 5 uM 40 mins Inhibition of Ca2+-induced mitochondrial permeability transition in human HL60 cells at 5 uM after 40 mins relative to control. 23026083
RPMI1788 Immunosuppressive assay 6 days Immunosuppressive activity in human RPMI1788 cells cocultured with human PBMC assessed as inhibition of [3H]thymidine incorporation incubated for 6 days prior to [3H]thymidine addition measured after 18 hrs by liquid scintillation counting, IC50 = 0.054 μM. 23347804
MT4 Antiviral assay 4 days Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay, EC50 = 0.45 μM. 23849880
A2780Adr Function assay 30 mins Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay, IC50 = 0.99 μM. 23851114
2008 Function assay 30 mins Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay, IC50 = 2.81 μM. 23851114
Jurkat T Function assay 30 mins Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay, IC50 = 0.0014 μM. 23964991
MDA435/LCC6MDR Function assay Modulation of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversal of paclitaxel resistance, EC50 = 0.032 μM. 24171478
MDA435/LCC6 Cytotoxicity assay 3 days Cytotoxicity against human MDA435/LCC6 cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 2.8 μM. 24171478
MDA435/LCC6MDR Cytotoxicity assay 3 days Cytotoxicity against human MDA435/LCC6MDR cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 8.3 μM. 24171478
L929 Cytotoxicity assay 3 days Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 33.9 μM. 24171478
A2780adr Function assay up to 90 mins Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay, IC50 = 0.92 μM. 24184213
2008 Function assay up to 90 mins Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay, IC50 = 2.7 μM. 24184213
Saos2 Function assay 5 uM 3 hrs Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as increase in doxorubicin uptake at 5 uM after 3 hrs by flow cytometric analysis. 24720452
Saos2 Function assay 5 uM 2 hrs Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as increase in intracellular doxorubicin retention at 5 uM after 2 hrs by flow cytometric analysis. 24720452
Saos2 Function assay 5 uM 2 to 3 hrs Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as intracellular doxorubicin distribution in nuclei at 5 uM after 2 to 3 hrs by laser scanning confocal microscopic analysis. 24720452
mouse Function assay Inhibition of human MDR1 expressed in mouse L5178 cells assessed as increase in intracellular accumulation of rhodamine 123 by FACSCalibur flow cytometry, IC50 = 0.67 μM. 24900226
A2780 Function assay 5 uM 40 mins Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in intracellular adriamycin level at 5 uM after 40 mins by flow cytometry analysis. 24900323
A2780 Function assay 5 uM 1 hr Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in adriamycin uptake at 5 uM after 1 hr by flow cytometry analysis. 24900323
A2780 Function assay 5 uM 8 hrs Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in adriamycin uptake at 5 uM after 8 hrs by flow cytometry analysis. 24900323
T-cells Antiinflammatory assay 0.01 to 100 nM 2 days Antiinflammatory activity in LLO118 TCR transgenic mouse IL-2-competent CD4-positive T cells assessed as inhibition of LLO (190 to 205)-induced IL-2 production at 0.01 to 100 nM for 2 days by flow cytometric analysis. 24900866
Th17 Antiinflammatory assay 10 to 100 nM 2 days Antiinflammatory activity in LLO118 TCR transgenic mouse Th17 cells assessed as inhibition of IL-17 production at 10 to 100 nM for 2 days by flow cytometric analysis. 24900866
Th1 Antiinflammatory assay 100 nM 2 days Antiinflammatory activity in LLO118 TCR transgenic mouse Th1 cells assessed as inhibition of IFN-gamma production at 100 nM for 2 days by flow cytometric analysis. 24900866
NCI/ADR-RES Function assay 20 mins Inhibition of human P-glycoprotein expressed in NCI/ADR-RES cells assessed as reduction of calcein-AM transport after 20 mins by fluorescence assay. 24992153
A2780adr Function assay 90 mins Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay, IC50 = 0.919 μM. 25855895
T spleen cells Cytotoxicity assay 72 hrs Cytotoxicity against ICR mouse T spleen cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.01 μM. 26564266
B spleen cells Cytotoxicity assay 72 hrs Cytotoxicity against ICR mouse B spleen cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.04 μM. 26564266
RD Antiviral assay 24 hrs Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay, EC50 = 3.66 μM. 26564266
mouse lymph node cells Function assay Inhibition of PI3K-gamma in mouse lymph node cells assessed as inhibition of ConA-stimulated T cell proliferation, IC50 = 0.57 μM. 26720154
CD1 Function assay 0.1 to 10 uM 30 mins Inhibition of taurolithocholate acid 3-sulfate-induced necrosis in CD1 mouse pancreatic acinar cells at 0.1 to 10 uM after 30 mins by propidium iodide staining based confocal microscopic analysis. 26950392
A2780/ADR Function assay 30 mins Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay, IC50 = 1.41 μM. 27100033
A2780/ADR Cytotoxicity assay 72 hrs Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay, GI50 = 8.63 μM. 27100033
A2780 Cytotoxicity assay 72 hrs Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay, GI50 = 8.94 μM. 27100033
MDCK2 Function assay Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry, IC50 = 25.6 μM. 27393949
Flp-InTM-293 Function assay 25 uM 30 mins Inhibition of ABCC2 (unknown origin) expressed in human Flp-InTM-293 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry. 27393949
hamster BHK21 Function assay 25 uM 30 mins Inhibition of human ABCC1 expressed in hamster BHK21 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins by flow cytometry. 27393949
MDCK2 Function assay 25 uM 30 mins Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry. 27393949
NH3T3 Function assay 2.5 uM 30 mins Inhibition of human ABCB1 expressed in mouse NH3T3 cells assessed as inhibition of calcein-AM efflux at 2.5 uM measured after 30 mins by flow cytometry. 27393949
Jurkat T Immunosuppressive assay 13 hrs Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA, IC50 = 0.011 μM. 27647370
A2780/ADR Function assay 30 mins Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay, IC50 = 1.21 μM. 27676469
MDA435/LCC6MDR Function assay 1 uM 5 days Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 1 uM measured after 5 days by Cell Titer 96 Aqueous assay (Rvb = 139.3 +/- 7.5 nM), IC50 = 0.0018 μM. 27750197
K562R Function assay 5 uM 1 hr Inhibition of P-gp in doxorubicin-resistant human K562R cells assessed as rhodamine efflux by measuring ratio of mean fluorescence intensity in presence and absence of compound at 5 uM incubated for 1 hr by flow cytometry. 27753480
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay, EC50 = 0.17 μM. 28075591
HepaRG Antiviral assay 16 hrs Antiviral activity against HBV infected in human HepaRG cells assessed as reduction in viral infection after 16 hrs, IC50 = 0.2 μM. 28383274
replicon 2A cells Function assay 72 hrs Inhibition of mTOR signaling pathway in (unknown origin) in sub-genomic replicon 2A cells assessed as reduction in phosphorylated rps6 protein levels up to 400 nM after 72 hrs by Western blot analysis. 28442256
A2780adr Function assay 30 mins Inhibition of ABCB1 in human A2780adr cells assessed as reduction in calcein AM levels preincubated for 30 mins followed by calcein AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay, IC50 = 1.21 μM. 28471656
H69AR Function assay 30 mins Inhibition of ABCC1 in human H69AR cells assessed as reduction in calcein AM levels preincubated for 30 mins followed by calcein AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay, IC50 = 2.97 μM. 28471656
A2780/ADR Function assay 30 mins Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured at 60 secs interval for 60 mins by fluorescence assay, IC50 = 1.21 μM. 28841513
H69AR Function assay 30 mins Inhibition of ABCC1 in human H69AR cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured at 60 secs interval for 60 mins by fluorescence assay, IC50 = 3.53 μM. 28841513
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells. 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells. 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells. 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells. 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells. 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells. 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells. 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells. 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells. 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells. 29435139
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
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells. 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells. 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells. 29435139
C57BL/6 mouse lymph node cells Immunosuppressive assay 24 hrs Immunosuppressive activity in C57BL/6 mouse lymph node cells after 24 hrs by MTT assay, IC50 = 0.5 μM. 29871844
HuH7 Antiviral assay 3 days Antiviral activity against HCV genotype 2a infected in human HuH7 cells after 3 days by dual-glo luciferase reporter gene assay, EC50 = 0.773 μM. 30074795
MT4 Cytotoxicity assay 4 to 5 days Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay, CC50 = 5.608 μM. 30074795
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Información química, almacenamiento y estabilidad

Peso molecular 1202.61 Fórmula

C62H111N11O12

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 59865-13-3 Descargar SDF Almacenamiento de soluciones madre

Sinónimos Cyclosporine A, Cyclosporine, Ciclosporin, CsA,NSC 290193 Smiles CCC1C(=O)N(CC(=O)N(C(C(=O)NC(C(=O)N(C(C(=O)NC(C(=O)NC(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N1)C(C(C)CC=CC)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C

Solubilidad

In vitro
Lote:

DMSO : 100 mg/mL (83.15 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 100 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

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)

mg/kg g μL

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
calcineurin
(Cell-free assay)
7 nM
In vitro

La Cyclosporin A se une a la ciclofilina (inmunofilina) en las células T, forma un complejo ciclina-este compuesto que se une e inhibe la calcineurina. Este químico inhibe la calcineurina con una IC50 de 7 nM, luego bloquea la translocación nuclear de NF-AT. También afecta a las mitocondrias al evitar que el MTP (poro de transición de permeabilidad mitocondrial) se abra con una IC50 de 39 nM.

Ensayo de quinasa
Ensayo phosphatase
Se adquieren calcineurina y calmodulina de cerebro bovino purificadas. Las mezclas de reacción con enzima purificada contienen 100 nM de calcineurina, 100 nM de calmodulina y 5 μM de fosfopéptido marcado con 32P, en 60 μl (volumen total) de tampón de ensayo que contiene 20 mM de Tris (pH 8), 100 mM de NaCl, 6 mM de MgCl2, 0,5 mM de ditiotreitol, 0,1 mg de albúmina de suero bovino por ml, y bien 0,1 mM de CaCl2 o 5 mM de EGTA. Las mezclas de reacción con lisados celulares contienen 20 μl de lisado sin diluir, 5 μM de fosfopéptido marcado con 32P y 40 μl de tampón de ensayo. Cuando se indica, las mezclas de reacción contienen 50 μM de péptido 412 o 413 y/o 500 nM de ácido okadaico, un inhibidor específico de las fosfatasas 1 y 2A; 500 nM de ácido okadaico son suficientes para la inhibición de las fosfatasas independientes de Ca2+, mientras que concentraciones más altas inhiben parcialmente también la actividad dependiente de Ca2+. Después de 15 min a 30°C, las reacciones se terminan con la adición de 0,5 ml de tampón de fosfato de potasio 100 mM (pH 7,0) que contiene 5% de ácido tricloroacético. El fosfato inorgánico libre se aísla por cromatografía de intercambio catiónico Dowex y se cuantifica por recuento por centelleo como se describe.
In vivo

Cyclosporin A es un agente inmunosupresor eficaz después de la administración parenteral u oral en ratones, ratas y cobayas. , se utiliza clínicamente en trasplantes de órganos para prevenir el rechazo.

Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/1715516/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8567677/
  • [6] https://pubmed.ncbi.nlm.nih.gov/328380/
  • [7] https://pubmed.ncbi.nlm.nih.gov/7520105/
  • [8] https://link.springer.com/chapter/10.1007/978-94-011-0679-5_12
  • [9] https://pubmed.ncbi.nlm.nih.gov/27725720/

Aplicaciones

Métodos Biomarcadores Imágenes PMID
Western blot Phospho-AKT1 / AKT1 / PTEN / Phospho-BAD / BAD / Procaspase-3 Cyp-D / AIF / β-actin IL-8 / MCP-1 Actin / Smac β-actin / FIPV-N
S2286-WB-1
12644839
Growth inhibition assay NPC death
S2286-Growth-inhibition-assay-1
20181586
IHC Th22 / Th17 / Th1 / M1 / Th2 Tregs / Bregs / pDCs / M2 Ki 67 / Fas-FasL IFN-γ / TNF-α WT-PCLS / FXRKO-PCLS
S2286-IHC-1
30916387
Immunofluorescence Human gingival fibroblast cells Human gingival fibroblast cells Calcein Rhod-Dex / Calcein cadherin-9 / vimentin
S2286-IF-1
27857765

Información del ensayo clínico

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

Número NCT Reclutamiento Condiciones Patrocinador/Colaboradores Fecha de inicio Fases
NCT06366685 Not yet recruiting
Esophageal Cancer|Exercise Training|Psychotherapy|Rehabilitation
Mengmeng Yuan|Anhui Medical University
 May 1 2024 Not Applicable
NCT06320561 Not yet recruiting
Stroke
Vrije Universiteit Brussel|University Ghent|Research Foundation Flanders
 May 2024 --
NCT05702931 Not yet recruiting
Hyperglycemia|Renal Transplant Complication Primary Non-Function|Diabetes
Rigshospitalet Denmark|Aarhus University Hospital|Odense University Hospital
 April 1 2024 Phase 4
NCT06052761 Recruiting
Child in Hospital
Adiyaman University
 February 10 2024 Not Applicable

Soporte técnico

Instrucciones de manipulación

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Preguntas frecuentes

Pregunta 1:
What is the difference between it (S2286) and S1514 (cyclosporin)?

Respuesta:
Cyclosporine is a mixture of Cyclosporine A, derivatives of Cyclosporine A, salts of Cyclosporine A. It is an especially useful component.