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PF-4981517

Catalog No.
A4311
CYP3A4 inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
5mg
$252.00
Ship with 5-10 days
10mg
$368.00
Ship with 5-10 days
25mg
$739.00
Ship with 5-10 days
50mg
$1,308.00
Ship with 5-10 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

PF-4981517, also named CYP3cide, is a potent, efficient, and specific time-dependent inactivator 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 compound's pharmacokinetics. PF-4981517 is a lipophilic compound with a pKa which will render it cationic at physiological pH. Thus, it is possible that if incubate with high concentrations of microsomes, it can nonspecifically partition into microsomal phospholipid, and its apparent potency will be reduced. PF-4981517 should be useful to investigators seeking to delineate the relative contribution of CYP3A4 versus CYP3A5 in the metabolism of compounds cleared by CYP3A.

Reference

Robert L. Walsky, R. Scott Obach, Ruth Hyland, Ping Kang, Sue Zhou, Michael West, Kieran F. Geoghegan, Christopher J. Helal, Gregory S. Walker, Theunis C. Goosen and Michael A. Zientek. Selective Mechanism-Based Inactivation of CYP3A4 by CYP3cide (PF-04981517) and Its Utility as an In Vitro Tool for Delineating the Relative Roles of CYP3A4 versus CYP3A5 in the Metabolism of Drugs. DMD September 2012 vol. 40 no. 9 1686-1697.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt456.59
Cas No.1390637-82-7
FormulaC26H32N8
SynonymsCYP3cide,PF-04981517,PF4981517
SolubilitySoluble in DMSO
Chemical Name1-methyl-3-[1-methyl-5-(4-methylphenyl)pyrazol-4-yl]-4-[(3S)-3-piperidin-1-ylpyrrolidin-1-yl]pyrazolo[3,4-d]pyrimidine
SDFDownload SDF
Canonical SMILESCC1=CC=C(C=C1)C2=C(C=NN2C)C3=NN(C4=C3C(=NC=N4)N5CCC(C5)N6CCCCC6)C
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description PF-4981517 is a potent and selective inhibitor of CYP3A4 with IC50 value of 30 nM.
Targets CYP3A4          
IC50 30 nM          

Quality Control

Quality Control & MSDS

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Chemical structure

PF-4981517