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    PF-4981517
    PF-4981517

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0816
    CAS #: 1390637-82-7Purity ≥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: Drug Metab Dispos. 2012 Sep;40(9):1686-97.

    Related CAS #: 1390637-82-7  

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    Molecular Weight (MW)456.59
    FormulaC26H32N8
    CAS No.1390637-82-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 91 mg/mL (199.3 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)

    Chemical Name: 1-Methyl-3-[1-methyl-5-(4-methylphenyl)-1H-pyrazol-4-yl]-4-[(3S)-3-piperidin-1-ylpyrrolidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine

    InChi Key: WDWIMDKOXZZYHH-FQEVSTJZSA-N

    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

    SMILES Code: CC1=CC=C(C2=C(C3=NN(C)C4=NC=NC(N5C[[email protected]@H](N6CCCCC6)CC5)=C43)C=NN2C)C=C1           

    SynonymsCYP3cide, PF-04981517; CYP3 cide, PF-4981517; PF 04981517; PF04981517, CYP-3cide, PF 4981517; PF4981517; 


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    In Vitro

    In vitro activity: 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.

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    References

    Drug Metab Dispos. 2012 Sep;40(9):1686-97.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    PF-4981517

    A, impact of CYP3cide (PF-4981517) on midazolam 1′-hydroxylase activity across a range of liver microsomes from genotyped donors. Drug Metab Dispos. 2012 Sep;40(9):1686-97. 

    PF-4981517

    Relationship between inhibition of midazolam 1′-hydroxylase activity and CYP3cide concentration in genotyped CYP3A5 *3/*3 HLM (HH101) at varying microsomal protein concentrations ranging from 0.1 to 10 mg/ml. Drug Metab Dispos. 2012 Sep;40(9):1686-97. 
     

    PF-4981517

    Impact of CYP3cide and ketoconazole on the consumption of midazolam (A), tacrolimus (B), and otenabant (C) in HLM from donors of genotyped CYP3A5 *1/*1 (red), *1/*3 (blue), and *3/*3 (yellow). Drug Metab Dispos. 2012 Sep;40(9):1686-97. 


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