名称 | BMS-564929 |
描述 | BMS-564929 is an agonist of androgen receptor (AR, Ki of 2.11±0.16 nM). |
体外活性 | 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. |
体内活性 | 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. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 50 mg/mL (163.55 mM), Sonication is recommended.
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关键字 | BMS-564929 | BMS564929 | BMS 564929 |
相关产品 | Dehydroisoandrosterone 3-acetate | Bicalutamide | 2,2,5,7,8-Pentamethyl-6-Chromanol | S-23 | Bavdegalutamide | Octinoxate | Adrenosterone | Allura Red AC | SK33 | Sunset Yellow FCF | Ostarine | Flutamide |