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BMS-564929Androgen receptor (AR) modulator

BMS-564929

Catalog No. A3251
Size Price Stock
5mg $299.00 Please Inquire
10mg $556.00 Please Inquire
50mg $1,520.00 Please Inquire
200mg $3,335.00 Please Inquire

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

BMS-564929

Biological Activity

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.
Targets androgen receptor          
IC50 2.11 nM (Ki)          

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Chemical Properties

Cas No. 627530-84-1 SDF Download SDF
Synonyms BMS 564929;BMS564929
Chemical Name 4-[(7R,7aS)-7-hydroxy-1,3-dioxo-5,6,7,7a-tetrahydropyrrolo[1,2-c]imidazol-2-yl]-2-chloro-3-methylbenzonitrile
Canonical SMILES CC1=C(C=CC(=C1Cl)C#N)N2C(=O)C3C(CCN3C2=O)O
Formula C14H12ClN3O3 M.Wt 305.72
Solubility Soluble in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

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 2.81 ± 0.48 nM measured for testosterone [1].
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 [1].
References:
[1]. 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.
[2]. 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.