02 BMS-564929 powder (627530-84-1) video
03 BMS-564929 powder Base Information
|Molecular Weight||305.72 g/mol|
|Melting Point||Not available|
|Half Life||Not available|
|Solubility||DMSO : 50 mg/mL (163.55 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
|Storage Condition||Store at -20°C|
|Application||BMS-564929 is a selective androgen receptor modulator that induces anabolic effects. Potential use in osteoporosis treatments.|
04 BMS-564929 powder General Description
BMS-564929 powder is a highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator. BMS-564929 is a subnanomolar AR agonist in vitro, is highly selective for the AR vs. other steroid hormone receptors, and exhibits no significant interactions with SHBG or aromatase. Dose response studies in castrated male rats show that BMS-564929 is substantially more potent than testosterone (T) in stimulating the growth of the levator ani muscle, and unlike T, highly selective for muscle vs. prostate.
05 BMS-564929 powder (627530-84-1) History
BMS-564,929 powder is an investigational selective androgen receptor modulator (SARM) which is being developed by Bristol-Myers Squibb for treatment of the symptoms of age-related decline in androgen levels in men (“andropause”). These symptoms may include depression, loss of muscle mass and strength, reduction in libido and osteoporosis. Treatment with exogenous testosterone is effective in counteracting these symptoms but is associated with a range of side effects, the most serious of which is enlargement of the prostate gland, which can lead to benign prostatic hypertrophy and even prostate cancer. This means there is a clinical need for selective androgen receptor modulators, which produce anabolic effects in some tissues such as muscle and bone, but without stimulating androgen receptors in the prostate.
06 BMS-564929 (627530-84-1) Mechanism Of Action
Description: BMS-564929 is an androgen receptor (AR) agonist, binds to androgen receptor (AR) with a Ki of 2.11±0.16 nM.
IC50 & Target: Ki: 2.11±0.16 nM (Androgen receptor)
In Vitro: 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.
In Vivo: 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 ED50 of 0.0009 mg/kg in the levator ani and an ED50 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.
07 BMS-564929 (627530-84-1) Application
BMS-564929 is a selective androgen receptor modulator that induces anabolic effects. Potential use in osteoporosis treatments.
08 BMS-564929 (627530-84-1) More Research
BMS-564,929 is one such compound currently in early human clinical trials, which is an orally active, potent and selective agonist for androgen receptors (Ki 2.1nM, 20x functional selectivity for muscle tissue over prostate) and in studies on castrated rats it was shown to counteract decrease in muscle mass over time, and at higher doses even increased muscle mass, without significantly affecting prostate tissue. It does however vastly reduce luteinizing hormone levels, it being an astonishing 33x more suppressive compound than testosterone, which may be a problem in human clinical use.
Selective androgen receptor modulators may also be used by athletes to assist in training and increase physical stamina and fitness, potentially producing effects similar to anabolic steroids but with significantly fewer side effects. For this reason, SARMs have already been banned by the World Anti-Doping Agency since January 2008 despite no drugs from this class yet being in clinical use, and blood tests for all known SARMs are currently being developed.
09 BMS-564929 (627530-84-1) Document Download
10 BMS-564929 (627530-84-1) Reference
- 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.
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. J Pharmacol Exp Ther. 2009 Feb;328(2):663-70.
- Ke, H. et al.: J. Musculoskelet. Neuronal. Interact., 5, 355 (2005); Vajda, E. et al.: J. Pharmacol. Exp. Ther., 328, 663 (2009);
- 01. Overview
- 02. BMS-564929 powder (627530-84-1) video
- 03. BMS-564929 powder Base Information
- 04. BMS-564929 powder General Description
- 05. BMS-564929 powder (627530-84-1) History
- 06. BMS-564929 (627530-84-1) Mechanism Of Action
- 07. BMS-564929 (627530-84-1) Application
- 08. BMS-564929 (627530-84-1) More Research
- 09. BMS-564929 (627530-84-1) Document Download
- 10. BMS-564929 (627530-84-1) Reference