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BMS-564929

Catalog No. T14675   CAS 627530-84-1

BMS-564929 is an agonist of androgen receptor (AR, Ki of 2.11±0.16 nM).

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BMS-564929 Chemical Structure
BMS-564929, CAS 627530-84-1
Pack Size Availability Price/USD Quantity
50 mg 6-8 weeks $ 717.00
100 mg 6-8 weeks $ 996.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BMS-564929 is an agonist of androgen receptor (AR, Ki of 2.11±0.16 nM).
Targets&IC50 Androgen receptor:(ki)2.11±0.16 nM
In vitro BMS-564929 exhibits high selectivity, being over 1000-fold more selective for androgen receptors (AR) compared to estrogen receptors (ER) α and β, glucocorticoid receptor (GR), and mineralocorticoid receptor (MR), with about 400-fold selectivity against progesterone receptor (PR). It demonstrates no measurable activity in functional transactivation assays involving ERα/β, GR, MR, or PR at concentrations up to 30 μM. Furthermore, BMS-564929 shows potent activity in the C2C12 myoblast cell line, with an EC50 (the concentration needed to achieve 50% of the maximum stimulatory effect of DHT) of 0.44±0.03 nM, and in the PEC cell line, the EC50 is 8.66±0.22 nM.
In vivo BMS-564929 demonstrates a significant enhancement in muscle stimulation potency, being over 200 times more effective than T propionate (TP) and 80 times more selective in targeting muscle versus prostate in the evaluated model[1]. Administered orally, BMS-564929 showcases superior efficacy in the levator ani muscle, with an ED50 of 0.0009 mg/kg, compared to its ED50 of 0.14 mg/kg in the prostate, indicating a notable 160-fold preference for muscle over prostate in sexually mature, castrated male rats—a thoroughly studied animal model. Remarkably, muscle stimulation peaks at approximately 100% with a dose of 0.1 mg/kg and exceeds 125% at higher doses of 0.3 and 1 mg/kg.
Molecular Weight 305.72
Formula C14H12ClN3O3
CAS No. 627530-84-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (163.55 mM), Sonification is recommended.

TargetMolReferences and Literature

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.

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Keywords

BMS-564929 627530-84-1 Endocrinology/Hormones Androgen Receptor BMS564929 BMS 564929 inhibitor inhibit

 

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