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Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources).1 It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms.1 Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.1,2
WARNING This product is not for human or veterinary use.
1. Highly selective inhibition of human CYP3Aa in vitro by azamulin and evidence that inhibition is irreversible. Drug Metab. Dispos. 32(1), 105-112 (2004).
2. Automated screening with confirmation of mechanism-