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 |



