product name PF-4981517
Description: PF-4981517, also named as CYP3cide and PF-04981517, is a potent, selective, efficient, and specific inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, it exhibits >500-fold selectivity over CYP3A5 and CYP3A7 and a time-dependent inactivation of human CYP3A4. PF-4981517 is a very useful tool for understanding the relative roles of CYP3A4 versus CYP3A5 and the impact of CYP3A5 genetic polymorphism on a compounds pharmacokinetics.
References: Drug Metab Dispos. 2012 Sep;40(9):1686-97.
456.59
Formula
C26H32N8
CAS No.
1390637-82-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 91 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
CYP3cide, PF-04981517
other peoduct :
| In Vitro |
In vitro activity: PF-4981517 (CYP3cide) is a potent, efficient, and specific time-dependent inactivator of human CYP3A4. PF-4981517 is tested as a reversible inhibitor of several human cytochrome P450 activities in pooled HLMs. PF-4981517 is selective for CYP3A4 with IC50 of 0.03 μM, 17 μM and 70 μM for CYP3A4, 3A5, and 3A7, respectively. PF-4981517 is a mechanism-based inactivator. PF-4981517 serves as an important in vitro tool, which when used side-by-side with ketoconazole to inhibit all CYP3A activity will permit distinction between the contribution of CYP3A4 to CYP3A5 (as well as CYP3A7 and maybe CYP3A43). PF-4981517 is useful to investigators seeking to delineate the relative contribution of CYP3A4 versus CYP3A5 in the metabolism of compounds cleared by CYP3A. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Drug Metab Dispos. 2012 Sep;40(9):1686-97. |
