Protein Information

Name CYP2C9
Synonyms (R) limonene 6 monooxygenase; Xenobiotic monooxygenase; Mephenytoin 4 hydroxylase; Microsomal monooxygenase; S mephenytoin 4 hydroxylase; (S) limonene 6 monooxygenase; (S) limonene 7 monooxygenase; CPC 9…

Compound Information

Name niclosamide
CAS

Reference List

PubMed Abstract RScore(About this table)
14557374 Egnell AC, Eriksson C, Albertson N, Houston B, Boyer S: Generation and evaluation of a CYP2C9 heteroactivation pharmacophore. J Pharmacol Exp Ther. 2003 Dec;307(3):878-87. Epub 2003 Oct 13.

Several potent heteroactivators of CYP2C9-mediated 7-methoxy-4-trifluoromethyl-coumarin metabolism are marketed drugs or endogenous compounds (amiodarone, niclosamide, liothyronine, meclofenemate, zafirlukast, estropipate, and dichlorphenamide, yielding 150% control reaction velocity at 0.04, 0.09, 0.5, 1, 1.2, 1.5, and 2.5 microM, respectively).
85(1,1,1,5) Details
11124226 Bapiro TE, Egnell AC, Hasler JA, Masimirembwa CM: Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metab Dispos. 2001 Jan;29(1):30-5.

Niclosamide had substrate-dependent contrasting effects on CYP2C9 activity with an apparent activation (400%) of 7-methoxy-4-trifluoromethylcoumarin demethylase activity and potent inhibition (K (i) = 6.00 microM) of diclofenac 4-hydroxylase activity.
81(1,1,1,1) Details