Cat. No. Name Size Price Add Cart
KI2500PF-049815171 mg$140
PF-049815175 mg$210
PF-0498151710 mg$336
PF-0498151750 mg$1072
PF-04981517100 mg$1716

Chemical Characteristic

Product NamePF-04981517
SynonymsN/A
CAS No.1390637-82-7
Molecular Weight 456.59
FormulaC26H32ClN8
Chemical Name1-methyl-3-[1-methyl-5-(4-methylphenyl)-1H-pyrazol-4-yl]-4-[(3S)-3-(1-piperidinyl)-1-pyrrolidinyl]-1H-pyrazolo[3,4-d]pyrimidine
Smilesc1nc2c(c(n1)N1C[C@H](CC1)N1CCCCC1)c(nn2C)c1cnn(c1c1ccc(cc1)C)C
Chemical Structure

Biological activities

PF-04981517 is a potent and specific time-dependent inactivator of human CYP3A4. PF-04981517 inhibits midazolam 1??hydroxylase activity with IC50s of 0.03, 17 and 70 mM for CYP3A4, CYP3A5, and CYP3A7, respectively.[1]

Protocols

In vitro, PF-04981517 is prepared in 50:50 acetonitrile/water.[1]

References

[1] Walsky RL, 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, 40(9): 1686-1697.

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