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PF-4981517

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PF-4981517
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Cat #: V0816 CAS #: 1390637-82-7 Purity ≥ 98%

Description: PF-4981517 (also named as PF 04981517; PF04981517, CYP-3cide, PF 4981517; PF4981517) is a specific and time-dependent inactivator of human CYP3A4 (P450) with IC50 of 0.03 μM, it exhibits >500-fold selectivity for inhibiting CYP3A4 over CYP3A5 and CYP3A7 and a time-dependent inactivation of human CYP3A4.

References: 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):1686-97.

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Molecular Weight (MW)456.59
Molecular FormulaC26H32N8
CAS No.1390637-82-7
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 91 mg/mL (199.3 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
SMILES CodeCC1=CC=C(C2=C(C3=NN(C)C4=NC=NC(N5C[C@@H](N6CCCCC6)CC5)=C43)C=NN2C)C=C1
SynonymsCYP3cide, PF-04981517; CYP3 cide, PF-4981517; PF 04981517; PF04981517, CYP-3cide, PF 4981517; PF4981517;
ProtocolIn VitroWhen investigating the inhibitory properties of CYP3cide, an extreme metabolic inactivation efficiency (kinact/KI) of 3300 to 3800 ml • min-1 • μmol-1 is observed using human liver microsomes from donors of nonfunctioning CYP3A5 (CYP3A5 *3/*3). This observed efficiency equated to an apparent KI between 420 and 480 nM with a maximal inactivation rate (kinact) equal to 1.6 min-1. When CYP3cide is tested at a concentration and preincubation time to completely inhibit CYP3A4 in a library of genotyped polymorphic CYP3A5 microsomes, the correlation of the remaining midazolam 1'-hydroxylase activity to CYP3A5 abundance is significant.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.1901 mL10.9507 mL21.9015 mL43.8030 mL
5mM0.4380 mL2.1901 mL4.3803 mL8.7606 mL
10mM0.2190 mL1.0951 mL2.1901 mL4.3803 mL
20mM0.1095 mL0.5475 mL1.0951 mL2.1901 mL
Quality Control Documentation
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Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O
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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.