Superiority
6-bromoandrostenedione
CAS:38632-00-7
Characteristics: White to almost white crystalline powder
A selective inhibitor of aromatase (estrogen synthetase) would be a
useful pharmacological to…
Details
6-bromoandrostenedione
CAS:38632-00-7
Characteristics: White to almost white crystalline powder
A selective inhibitor of aromatase (estrogen synthetase) would be a
useful pharmacological tool with potential therapeutic application. We
have found that 6 alpha-bromoandrostenedione (6 alpha-BrA) is a
competitive inhibitor of human placental aromatase with respect to
androstenedione, with an apparent Ki of 3.4 nM, while 6 beta-BrA is a
mechanism-based irreversible inhibitor with an apparent Ki of 0.8
microM and a kinact of 0.025 min-1. Aromatase activity was measured by
tritium release into water from the 1 beta position of [1(-3)H,4(-14)
C]androstenedione in reaction mixtures containing NADPH and the
aromatase.