A potent, selective inhibitor of CYP3A4
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PF-04981517

Item No. 15019

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-methyl-3-[1-methyl-5-(4-methylphenyl)-1H-pyrazol-4-yl]-4-[(3S)-3-(1-piperidinyl)-1-pyrrolidinyl]-1H-pyrazolo[3,4-d]pyrimidine
CAS Number
1390637-82-7
Synonyms
  • CYP3cide
Molecular Formula
C26H32N8
Formula Weight
456.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 2 mg/ml
λmax
203, 295 nm
SMILES
CC1=CC=C(C2=C(C3=NN(C)C4=C3C(N5C[C@@H](N6CCCCC6)CC5)=NC=N4)C=NN2C)C=C1
InChi Code
InChI=1S/C26H32N8/c1-18-7-9-19(10-8-18)24-21(15-29-31(24)2)23-22-25(32(3)30-23)27-17-28-26(22)34-14-11-20(16-34)33-12-5-4-6-13-33/h7-10,15,17,20H,4-6,11-14,16H2,1-3H3/t20-/m0/s1
InChi Key
WDWIMDKOXZZYHH-FQEVSTJZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $95

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    10 mg

    $178

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    25 mg

    $417

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    50 mg

    $739

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    Product Description

    PF-04981517 is a potent, time-dependent inhibitor of the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 30 nM).1 It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 μM, respectively).1 PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Walsky, R.L., Obach, R.S., Hyland, R., et al. Selective mechanism-based inactivation of cytochrome P4503A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of cytochrome P4503A4 versus P4503A5 in the metabolism of drugs. Drug Metab. Dispos. 40(9), 1686-1697 (2012).