BMS-564929 is an agonist of androgen receptor (AR, Ki of 2.11±0.16 nM).

Androgen receptor:（ki）2.11±0.16 nM

BMS-564929 exhibits high selectivity, being over 1000-fold more selective for androgen receptors (AR) compared to estrogen receptors (ER) α and β, glucocorticoid receptor (GR), and mineralocorticoid receptor (MR), with about 400-fold selectivity against progesterone receptor (PR). It demonstrates no measurable activity in functional transactivation assays involving ERα/β, GR, MR, or PR at concentrations up to 30 μM. Furthermore, BMS-564929 shows potent activity in the C2C12 myoblast cell line, with an EC50 (the concentration needed to achieve 50% of the maximum stimulatory effect of DHT) of 0.44±0.03 nM, and in the PEC cell line, the EC50 is 8.66±0.22 nM.

BMS-564929 demonstrates a significant enhancement in muscle stimulation potency, being over 200 times more effective than T propionate (TP) and 80 times more selective in targeting muscle versus prostate in the evaluated model[1]. Administered orally, BMS-564929 showcases superior efficacy in the levator ani muscle, with an ED50 of 0.0009 mg/kg, compared to its ED50 of 0.14 mg/kg in the prostate, indicating a notable 160-fold preference for muscle over prostate in sexually mature, castrated male rats—a thoroughly studied animal model. Remarkably, muscle stimulation peaks at approximately 100% with a dose of 0.1 mg/kg and exceeds 125% at higher doses of 0.3 and 1 mg/kg.