HighaffinityP-glycoprotein(P-gp)inhibitor(Kivaluesare58and94nMformousePgp1aandPgp1bisoforms).Inhibitscalcein-AMuptakeinMDR1-transfectedMDCKIIcells(IC50=0.5μM)andprazosintransportinBCRP-transfectedMDCKIIcells(IC50=1.5μM).DisplaysweakornoinhibitoryactivityagainstMRP1,OATP1B1andseveralmajorhumanP450enzymes(IC50>50μM).
SoldforresearchpurposesunderagreementfromPfizerInc.
M.Wt | 597.1 |
Formula | C31H36N4O6.HCl |
Storage | DesiccateatRT |
Purity | ≥98%(HPLC) |
CASNumber | 142715-48-8 |
PubChemID | 71312025 |
InChIKey | WWCHXVYTCMPAMV-UHFFFAOYSA-N |
Smiles | COC2=CC1=C(N3CCC(C=C(OC)C(OC)=C5)=C5C3)N=C(NCCC4=CC=C(OC)C(OC)=C4)N=C1C=C2OC.Cl |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Solvent | MaxConc.mg/mL | MaxConc.mM | |
---|---|---|---|
Solubility | |||
DMSO | 11.94 | 20 |
Thefollowingdataisbasedontheproductmolecularweight597.1.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
---|---|---|---|
1mM | 1.67mL | 8.37mL | 16.75mL |
5mM | 0.33mL | 1.67mL | 3.35mL |
10mM | 0.17mL | 0.84mL | 1.67mL |
50mM | 0.03mL | 0.17mL | 0.33mL |