Potent, selective human type 1 5α-reductase inhibitor
Potent and selective human type 1 5α-reductase inhibitor (5αR1, IC50 = 0.9 nM). Exhibits 100-fold selectivity for 5αR1 over 5αR2 (IC50 = 154 nM). Supresses human serum and sebum dihydrotestosterone (DHT) levels in a dose-dependent manner without affecting semen DHT concentrations. Orally active.
Schwartz et al (1997) MK-386, an inhibitor of 5α-reductase type 1, reduces dihydrotestosterone concentrations in serum and sebum without affecting dihydrotestosterone concentrations in semen. J.Clin.Endocrinol.Metab. 82 1373 PMID:9141518 |Bakshi et al (1994) 4,7 beta-Dimethyl-4-azacholestan-3-one (MK-386) and related 4-azasteroids as selective inhibitors of human type 1 5 alpha-reductase. J.Med.Chem. 37 3871 PMID:7966146
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