BMS-564929 是一种 雄激素受体 (AR) 激动剂，结合到雄激素受体，K_i 为 2.11±0.16 nM。

BMS-564929 is an androgen receptor (AR) agonist, binds to androgen receptor (AR) with a K i of 2.11±0.16 nM.

Solid

Ki: 2.11±0.16 nM (Androgen receptor)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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 ED 50 of 0.0009 mg/kg in the levator ani and an ED 50 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Ostrowski J, et al. Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats. Endocrinology. 2007 Jan;148(1):4-12.

In Vitro: DMSO : 50 mg/mL (163.55 mM; Need ultrasonic)配制储备液