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PF-4981517

Name: PF-4981517
Brand: Selleck Chemicals
SKU: S2921
Rating: 5 (1 reviews)

Synonyms: CYP3cide, PF-04981517

Catalog No.S2921 Purity: 99.93%

PF-4981517 (CYP3cide, PF-04981517) is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.

PF-4981517 Chemical Structure

CAS: 1390637-82-7

Purity & Quality Control

Batch: S292150 DMSO] 91 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.93%

99.93

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Signaling Pathway

P450 (e.g. CYP17) Signaling Pathway

Choose Selective P450 (e.g. CYP17) Inhibitors

Biological Activity

Description

PF-4981517 (CYP3cide, PF-04981517) 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
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]

References

[1] Walsky RL, et al. Drug Metab Dispos, 2012, 40(9), 1686-1697.

Chemical Information & Solubility

Molecular Weight	456.59	Formula	C₂₆H₃₂N₈
CAS No.	1390637-82-7	SDF	Download PF-4981517 SDF
Smiles	CC1=CC=C(C=C1)C2=C(C=NN2C)C3=NN(C4=C3C(=NC=N4)N5CCC(C5)N6CCCCC6)C
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 91 mg/mL ( (199.3 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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