PF-4981517

Licensed and Manufactured by Pfizer Catalog No.S2921 Synonyms: CYP3cide, PF-04981517

PF-4981517 Chemical Structure

Molecular Weight(MW): 456.59

PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.

Size Price Stock Quantity  
In DMSO USD 270 In stock
USD 210 In stock
USD 670 In stock
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Biological Activity

Description PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.
Targets
CYP3A4 [1]
30 nM
In vitro

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. [1]

Protocol

Solubility (25°C)

In vitro DMSO 91 mg/mL (199.3 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 456.59
Formula

 

C26H32N8
 
CAS No. 1390637-82-7
Storage powder
in solvent
Synonyms CYP3cide, PF-04981517

Bio Calculators

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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P450 (e.g. CYP17) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID