BMS 564929, Androgen receptor (AR) modulator

New Drug Approvals



BMS-564929; BMS564929; 627530-84-1; 2-Chloro-4-[(7r,7as)-7-Hydroxy-1,3-Dioxotetrahydro-1h-Pyrrolo[1,2-C]imidazol-2(3h)-Yl]-3-Methylbenzonitrile; hydantoin,

CAS 627530-84-1Squibb Bristol Myers Co

Molecular Formula:C14H12ClN3O3
Molecular Weight:305.71638 g/mol


7-K,7aS)-2-Chloro-4-(7-hydroxy-l,3-dioxotetrahydropyrrolo[l,2- c]imidazol-2-yl)-3-methylbenzonitrile


BMS-564929 is a highly potent, orally active and nonsteroidal tissue selective modulator of androgen receptor (AR) with Ki value of 2.11 nM.

BMS-564929 is a selective androgen receptor (AR) modulator with Ki value of 2.11 ± 0.16 nM [1].
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 [2]. 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…

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