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PF-4981517

Catalog No. T21548 CAS 1390637-82-7

Synonyms: CYP3cide

PF-4981517 (CYP3cide) is a efficient, specific and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC 50 values for CYP3A activity are 0.03 μM,17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. PF-4981517 is able to be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug Metabolism.

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PF-4981517, CAS 1390637-82-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 312.00
50 mg	In stock	Inquiry

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Purity: 99.77%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

In vitro

Investigating CYP3cide's ability to inhibit, it exhibits an outstanding metabolic inactivation efficiency (k inact /K I ) ranging from 3300 to 3800 ml min^-1 μmol^-1 in human liver microsomes of donors with nonfunctional CYP3A5 (CYP3A5 *3/*3). This efficiency corresponds to an apparent KI of 420 to 480 nM and a maximum inactivation rate (kinact) of 1.6 min^-1. In experiments where CYP3cide is applied at concentrations and preincubation times sufficient to fully inhibit CYP3A4 across a range of genotypically distinct CYP3A5 microsomes, a significant correlation between remaining CYP3A activity and CYP3A5 presence is observed.

Synonyms	CYP3cide
Molecular Weight	456.59
Formula	C26H32N8
CAS No.	1390637-82-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 9 mg/mL (19.7 mM), Sonication and heating to 60℃ are recommended.

References and Literature

1. Robert L Walsky, et al. 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. Drug Metab Dispos. 2012 Sep;40(9)

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max Anti-Metabolism Disease Compound Library Bioactive Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PF-4981517 1390637-82-7 Metabolism P450 PF 4981517 PF4981517 CYP3cide inhibitor inhibit

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