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Tariquidar (XR9576) P-gp remmer

Name: Tariquidar (XR9576)
Brand: Selleck Chemicals
SKU: S8028
Rating: 5 (54 reviews)

Cat.Nr.S8028

Tariquidar is een potente en selectieve niet-competitieve remmer van P-glycoproteïne met een K_d van 5,1 nM in de CHrB30-cellijn, keert medicijnresistentie om in MDR-cellijnen. Fase 3.

Tariquidar (XR9576) P-gp remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 646.73

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Kwaliteitscontrole

Batch: Zuiverheid: 99.81%

99.81

Gerelateerde doelwitten	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase
Overige P-gp Inhibitoren	Zosuquidar 3HCl Elacridar (GF120918) (20S)-Protopanaxadiol Solamargine Sinapine Levistilide A Evodine Valspodar Wilforine Encequidar (HM30181)

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
K562/DOX	Function assay	1 uM	10 mins	Inhibition of P-gp in human K562/DOX cells assessed as increase in rhodamine-123 efflux in human K562 cells at 1 uM incubated for 10 mins hrs by flow cytometry relative to untreated control	28113128
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
KB-V1	Function assay	200 nM		Inhibition of P-gp in human KB-V1 cells assessed as increase in rhodamine 123 accumulation at 200 nM	21657271
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
HepG2	Cytotoxicity assay		48 hrs	Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50=37.2μM	27328029
K562	Cytotoxicity assay		48 hrs	Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50=31.56μM	28645831
K562	Cytotoxicity assay		48 hrs	Cytotoxicity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=31.56μM	29631786
A2780adr	Function assay	10 uM	30 mins	Inhibition of ABCB1 in human A2780adr cells assessed as increase in accumulation of calcein AM at 10 uM preincubated for 30 mins followed by calcein AM addition measured every 60 secs for 60 mins by fluorescence assay relative to control	29547272
K562/A02	Cytotoxicity assay		48 hrs	Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=27.19μM	29631786
CCD-18Co	Cytotoxicity assay		48 hrs	Cytotoxicity against human CCD-18Co cells assessed as cell viability after 48 hrs by MTT assay, IC50=25μM	26197160
SW620/AD300	Cytotoxicity assay		48 hrs	Cytotoxicity against human SW620/AD300 cells assessed as cell viability after 48 hrs by MTT assay, IC50=25μM	26197160
HLF	Cytotoxicity assay		48 hrs	Cytotoxicity against HLF cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50=16.69μM	27328029
CEM/VLB500	Growth inhibition assay		3 days	Growth inhibition of human CEM/VLB500 cells after 3 days by resazurin assay, GI50=13.5μM	17399990
MCF7/ADR	Cytotoxicity assay		48 hrs	Intrinsic cytotoxicity against human MCF7/ADR cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50=13.1μM	27328029
HCT116	Cytotoxicity assay		48 hrs	Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay, IC50=12.5μM	26197160
K562/A02	Function assay		48 hrs	Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 12 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=8.28μM	28645831
KBV	Function assay	5 uM	72 hrs	Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of cytotoxicity by measuring IC50 at 5 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM), IC50=5.24μM	30384042
K562/A02	Function assay		48 hrs	Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 6 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=4.97μM	28645831
KBV	Function assay	10 uM	72 hrs	Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of cytotoxicity by measuring IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM), IC50=4.46μM	30384042
K562/A02	Function assay		48 hrs	Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured immediately by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=3.02μM	28645831
K562/A02	Function assay	5 uM	48 hrs	Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 43.75 to 96.91 uM), IC50=1.97μM	28645831
K562/A02	Function assay		48 hrs	Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 measured after 48 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=1.6μM	28645831
MCF-7 MX	Function assay			Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=1.5μM	21354800
MCF7	Function assay			Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay, IC50=1.44544μM	18678495
HFE	Cytotoxicity assay		72 hrs	Cytotoxicity against human HFE cells assessed as cell viability after 72 hrs by MTT assay, IC50=1.28μM	26197160
MDCK	Function assay			Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=0.94μM	21354800
MCF7/Topo	Function assay			Inhibition of ABCG2 overexpressed in human MCF7/Topo cells by flow cytometric-based mitoxantrone efflux assay, IC50=0.916μM	19170519
MCF7/Topo	Function assay		2 hrs	Inhibition of ABCG2 in human MCF7/Topo cells after 2 hrs by Hoechst 33342 staining based fluorescence assay, IC50=0.526μM	30128080
MCF7/Topo	Function assay		2 hrs	Inhibition of ABCG2 in human MCF7/Topo cells after 2 hrs by Hoechst 33342 microplate assay, IC50=0.526μM	24900683
MCF7/Topo	Function assay			Inhibition of ABCG2 expressed in human MCF7/Topo cells by Hoechst microplate assay, IC50=0.526μM	21570282
MCF7/Topo	Function assay			Inhibition of ABCG2 in human MCF7/Topo cells by Hoechst 33342 assay, IC50=0.52μM	26774038
KBV1	Function assay		10 mins	Inhibition of ABCB1 in human KBV1 cells after 10 mins by Calcein-AM microplate assay, IC50=0.223μM	24900683
Kb-V1	Function assay		10 mins	Inhibition of ABCB1 expressed in Kb-V1 cells after 10 mins by calcein-AM assay, IC50=0.223μM	21570282
KBv1	Function assay			Inhibition of ABCB1 overexpressed in human KBv1 cells by flow cytometric-based calcein-AM efflux assay, IC50=0.223μM	19170519
KBV1	Function assay			Inhibition of ABCB1 in human KBV1 cells assessed as inhibition of calcein-AM efflux, IC50=0.22μM	26774038
A2780	Function assay		30 mins	Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay, IC50=0.12589μM	18083034
KB-3-1	Function assay	1000 nM	72 hrs	Potentiation of doxorubicin-induced cytotoxicity against human KB-3-1 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.15 +/- 0.04 uM), IC50=0.11μM	27504669
OVCAR8	Function assay	1000 nM	72 hrs	Potentiation of doxorubicin-induced cytotoxicity against human OVCAR8 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.12 +/- 0.03 uM), IC50=0.08μM	27504669
A2780/ADR	Function assay			Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay, IC50=0.078μM	19250834
A2780adr	Function assay			Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay, IC50=0.08μM	21354800
A2780	Function assay			Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50=0.07244μM	18678495
KBV1	Function assay	1000 nM	72 hrs	Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 5.07 +/- 0.19 uM), IC50=0.07μM	27504669
CEM/VLB500	Function assay		3 days	Reversal of P-gp-mediated multidrug resistance to in human CEM/VLB500 cells after 3 days by resazurin assay, EC50=0.068μM	17399990
EMT6/AR1.0	Function assay		1 hr	Inhibition of mouse Pgp in EMT6/AR1.0 cells after 1 hr by daunorubicin accumulation assay, IC50=0.06457μM	18083034
EMT6/AR1.0	Function assay		1 hr	Inhibition of mouse Pgp in EMT6/AR1.0 cells after 1 hr by daunorubicin accumulation assay, IC50=0.064μM	18083034
MDCK	Function assay		30 mins	Inhibition of P-glycoprotein (unknown origin) expressed in MDCK cells assessed as reduction of calcein-AM transport after 30 mins by fluorescence assay, EC50=0.044μM	24607999
MDCK	Function assay		30 mins	Activity at MDR1 (unknown origin) expressed in MDCK cells using calcein AM as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis, EC50=0.044μM	23374872
NCI-ADR-RES	Function assay	1000 nM	72 hrs	Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of cytotoxicity by measuring IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 3714.80 +/- 383.58 nM), IC50=0.01851μM	27504669
KBV1	Function assay	1000 nM	72 hrs	Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of cytotoxicity by measuring IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 277.68 +/- 56.61 nM), IC50=0.00066μM	27504669
HEK293	Function assay	1000 nM	72 hrs	Potentiation of doxorubicin-induced cytotoxicity against HEK293 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by CCK8 assay (Rvb = 5.28 +/- 0.74 nM), IC50=0.00495μM	27504669
K562/A02	Cytotoxicity assay		48 hrs	Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay, IC50=27.19μM	28645831
SW620	Cytotoxicity assay		48 hrs	Cytotoxicity against human SW620 cells assessed as cell viability after 48 hrs by MTT assay, IC50=25μM	26197160
K562/A02	Function assay		48 hrs	Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 24 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=14.39μM	28645831
MDCK	Function assay			Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay, IC50=0.85μM	19932960
MCF7 MX	Function assay			Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining, IC50=0.68μM	19932960
NCI-ADR-RES	Function assay	1000 nM	72 hrs	Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 5.54 +/- 0.60 uM), IC50=0.24μM	27504669
MDCK	Function assay			Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry, IC50=0.21μM	21354800
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=0.03311μM	22452412
HEK293	Function assay	1000 nM	72 hrs	Inhibition of human ABCB1 transfected in HEK293 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by CCK8 assay (Rvb = 504.65 +/- 44.94 nM), IC50=0.02477μM	27504669
KB-3-1	Function assay	1000 nM	72 hrs	Potentiation of cytotoxicity against human KB-3-1 cells assessed as IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.78 +/- 0.27 nM), IC50=0.00041μM	27504669
OVCAR8	Function assay	1000 nM	72 hrs	Potentiation of cytotoxicity against human OVCAR8 cells assessed as IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 8.53 +/- 1.95 nM), IC50=0.00518μM	27504669
MDCK	Function assay		30 mins	Activity at BCRP (unknown origin) expressed in MDCK cells using rhodamine 123 as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis, EC50=0.01μM	23374872
HepG2	Function assay	10 uM	90 mins	Inhibition of P-gp mediated efflux in adriamycin-resistant human HepG2 cells assessed as intracellular rhodamine-123 accumulation at 10 uM incubated in dark condition for 90 mins by flow cytometry relative to control	27328029
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	646.73	Formule	C₃₈H₃₈N₄O₆	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	206873-63-4	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	XR9576			Smiles	COC1=C(C=C2CN(CCC2=C1)CCC3=CC=C(C=C3)NC(=O)C4=CC(=C(C=C4NC(=O)C5=CC6=CC=CC=C6N=C5)OC)OC)OC

Oplosbaarheid

In vitro
Batch:

DMSO : 8 mg/mL (12.36 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	0.280mg/ml (0.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 5.6 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.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	P-gp (CHrB30 cells) 5.1 nM(Kd)
In vitro	Tariquidar vertoont een hoge affiniteitsbinding aan P-gp met B_max van 275 pmol/mg. Deze verbinding vertoont een niet-competitieve interactie met de P-gp-substraten. Het verhoogt de steady-state accumulatie van deze cytotoxica in CH^rB30-cellen tot niveaus die waargenomen worden in niet-P-gp-expressende AuxB1-cellen met een EC50 van 487 nM. Deze chemische stof is in staat om de vanadaatgevoelige ATPase-activiteit van P-gp met 60-70% te remmen, met potente IC50-waarden van 43 nM. Het kan andere resistentiemechanismen bij hogere concentraties remmen. 1 μM van deze verbinding onderdrukt ABCG2 (BCRP)-gemedieerde resistentie tegen camptothecins in vitro. Het potentiëert de cytotoxiciteit van verschillende geneesmiddelen, waaronder doxorubicine; volledige omkering van resistentie wordt bereikt in aanwezigheid van 25-80 nM van deze chemische stof. In MC26, een murine darmcarcinoomcellijn met intrinsieke chemoresistentie, is de doxorubicine IC50 vijfvoudig lager in aanwezigheid van 0,1 μM van deze verbinding (36 vs 7 nM). In murine borstcarcinoom-, humane kleincellige longcarcinoom- en humane eierstokkarcinoomcellijnen met verworven chemotherapeutische resistentie (EMT6/AR1.0, H69/LX4 en 2780 AD), is de in vitro doxorubicine IC50 22-150-voudig lager in aanwezigheid van 0,1 μM van deze chemische stof. P-gp-remming houdt 23 uur aan na verwijdering ervan uit het kweeksysteem. Het herstelde de cytotoxiciteit van doxorubicine in het National Cancer Institute (NCI)/ADR^RES multicellulair tumor-sferoïdemodel, afgeleid van de MCF7^WT borstkankercellijn.
Kinase Assay	Steady-state geneesmiddelenaccumulatietest
Kinase Assay	Cellen worden geïncubeerd in een reactievolume van 1 mL gedurende 60 min bij 37 ℃ onder 5% CO₂ om een steady-state te bereiken. Het effect van de modulatoren XR9576 op [³H]-ligandaccumulatie wordt onderzocht in het concentratiebereik 10^-9 - 10^-6 M. Deze verbinding wordt toegevoegd uit een DMSO-stock, wat een uiteindelijke oplosmiddelconcentratie van 0,2% (v/v) oplevert. Na het oogsten van de cellen wordt het geaccumuleerde geneesmiddel gemeten door vloeistofscintillatietelling en genormaliseerd voor het celeiwitgehalte. Grafieken van de geaccumuleerde hoeveelheid als functie van de modulatorconcentratie worden gefit met de algemene dosis-responsvergelijking: Y={(a-b)/(1+(X/c)^d)}+bWaarbij: Y=respons; a=initiële respons; b=uiteindelijke respons; c=EC50-concentratie; d=hellingswaarde; X=geneesmiddelconcentratie.
In vivo	Tariquidar (2-8 mg/kg p.o.) blijkt de antitumoractiviteit van doxorubicine (5 mg/kg, i.v.) tegen MC26 murine coloncarcinoom in vivo significant te potentiëren. In menselijke carcinoomxenografts herstelde gelijktijdige toediening van deze verbinding (6-12 mg/kg p.o.) de antitumoractiviteit tegen twee zeer resistente MDR menselijke tumorxenografts (2780AD, H69/LX4) bij naaktmuizen volledig.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/10510451/ [2] https://pubmed.ncbi.nlm.nih.gov/14973080/ [3] https://pubmed.ncbi.nlm.nih.gov/11212278/ [4] https://pubmed.ncbi.nlm.nih.gov/14962729/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	PMID
Immunofluorescence	MRP7		23393594

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT01663545	Completed	Epilepsies Partial	National Institute of Neurological Disorders and Stroke (NINDS)\|National Institutes of Health Clinical Center (CC)	July 31 2012	--
NCT01547754	Terminated	HIV-Associated Cognitive Motor Complex	National Institute of Mental Health (NIMH)\|National Institutes of Health Clinical Center (CC)	January 9 2012	--
NCT01386476	Completed	Drug Resistance	National Institute of Mental Health (NIMH)\|National Institutes of Health Clinical Center (CC)	June 15 2011	--
NCT00082368	Completed	Cancer	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	May 16 2004	Phase 2

Technische ondersteuning

Gebruiksaanwijzing

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

Als u nog andere vragen heeft, kunt u een bericht achterlaten.

Veelgestelde vragen

Vraag 1:
Can you please give me more specific and detailed information of how to dissolve and use it (S8028) for in vivo studies?

Antwoord:
It in 30% Propylene glycol, 5% Tween 80, 65% D5W at 30mg/ml will be a suspension or emulsion. If you are going to administrate this compound by oral gavage, it is fine. We also have test some vehicles for it for i.p injection, and it is soluble in 5% DMSO+45% PEG 300+ddH2O at 2mg/ml clearly. When preparing the solution, please dissolve it in DMSO clearly first, then add PEG. After they mixed well, then dilute with water.

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