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- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
627530-84-1
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/50 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1540.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥636.0 |
| 规格: | 5 mg | 产品价格: | ¥1400.0 |
| 规格: | 10 mg | 产品价格: | ¥2300.0 |
| 规格: | 50 mg | 产品价格: | ¥9300.0 |
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BMS-564929
CAS No. : 627530-84-1
MCE 国际站:BMS-564929
产品活性:BMS-564929 是一种 雄激素受体 (AR) 激动剂,结合到雄激素受体,Ki 为 2.11±0.16 nM。
研究领域:Vitamin D Related/Nuclear Receptor
作用靶点: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.
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