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.
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All Tocris products are intended for laboratory research use only.
MK-386, an inhibitor of 5α-reductase type 1, reduces dihydrotestosterone concentrations in serum and sebum without affecting dihydrotestosterone concentrations in semen.
Schwartz et al.
4,7 beta-Dimethyl-4-azacholestan-3-one (MK-386) and related 4-azasteroids as selective inhibitors of human type 1 5 alpha-reductase.
Bakshi et al.