|BMS-564929Androgen receptor (AR) modulator|
Sample solution is provided at 25 µL, 10mM.
Publications citing ApexBio Products
|Description||BMS-564929 is a highly potent, orally active and nonsteroidal tissue selective modulator of androgen receptor (AR) with Ki value of 2.11 nM.|
|IC50||2.11 nM (Ki)|
|Cas No.||627530-84-1||SDF||Download SDF|
|Solubility||Soluble in DMSO||Storage||Store at -20°C|
BMS-564929 is a selective androgen receptor (AR) modulator with Ki value of 2.11 ± 0.16 nM .
The AR is a type of nuclear receptor that is activated by the androgenic hormones, testosterone, or dihydrotestosterone. The important function is regulating gene expression.
BMS-564929 is a muscle-tissue specific agonist for AR with a bicyclic hydantoin structure . BMS-564929 is about 400-fold selective for AR vs. PR and more than 1000-fold selective for AR vs. GR, MR and ERα and β. In the C2C12 myoblast cell line, BMS-564929 shows a potency of 0.44 ± 0.03 nM compared with 2.81 ± 0.48 nM measured for testosterone .
In castrated male rats, BMS-564929 is substantially more potent than testosterone (T) in promoting the growth of the levator ani muscle, and is highly selective for muscle vs. Prostate. Because of its potent oral activity and tissue selectivity, BMS-564929 is expected to yield beneficial clinical effects in muscle and other tissues with a more favorable safety way .
. Ostrowski J, Kuhns JE, Lupisella JA, 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, 148(1): 4-12.
. Thevis M, Kohler M, Thomas A, et al. Determination of benzimidazole- and bicyclic hydantoin-derived selective androgen receptor antagonists and agonists in human urine using LC-MS/MS. Anal Bioanal Chem, 2008, 391(1): 251-261.