BMS-564929

BMS-564929 is an androgen receptor (AR) agonist, binds to androgen receptor (AR) with a K_i of 2.11±0.16 nM. IC50 & Target: Ki: 2.11±0.16 nM (Androgen receptor)^[1] In Vitro: BMS-564929 exhibits a potency (EC₅₀, calculated as the concentration at which 50% of the maximum stimulatory effect of DHT is achieved) of 0.44±0.03 nM in the C2C12 myoblast cell line. In the PEC cell line, the EC₅₀ for BMS-564929 is 8.66±0.22 nM. BMS-564929 is more than 1000-fold selective for AR vs. estrogen receptors (ER) α and β, glucocorticoid receptor (GR), and mineralocorticoid receptor (MR), and approximately 400-fold selective vs. progesterone receptor (PR). BMS-564929 shows no measurable activity in functional transactivation assays with ERα/β, GR, MR, or PR at concentrations up to 30 μM^[1]. In Vivo: In sexually mature, castrated male rats, a well-characterized animal model, BMS-564929 (p.o.) shows substantially more potent activity in the levator ani, exhibiting an ED₅₀ of 0.0009 mg/kg in the levator ani and an ED₅₀ of 0.14 mg/kg in the prostate; a net 160-fold selectivity for muscle vs. prostate. Approximately 100% muscle stimulation is achieved at 0.1 mg/kg, reaching greater than 125% stimulation at 0.3 and 1 mg/kg. Compared with T propionate (TP) in the same model, BMS-564929 is more than 200 times more potent in stimulation of muscle and 80 times more selective for muscle vs. prostate^[1].