BMS-564929|cas:627530-84-1|西域试剂

BMS-564929,99.07%

产品编号：Bellancom-12111| CAS NO：627530-84-1| 分子式：C₁₄H₁₂ClN₃O₃| 分子量：305.72

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-12111	￥1400.00	杭州北京（现货）
Bellancom-12111	￥2300.00	杭州北京（现货）
Bellancom-12111	￥9300.00	杭州北京（现货）

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BMS-564929

产品介绍

BMS-564929 是一种 雄激素受体 (AR) 激动剂，结合到雄激素受体，K_i 为 2.11±0.16 nM。

生物活性

BMS-564929 is an androgen receptor (AR) agonist, binds to androgen receptor (AR) with a K_i of 2.11±0.16 nM.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (163.55 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2710 mL	16.3548 mL	32.7097 mL
5 mM	0.6542 mL	3.2710 mL	6.5419 mL
10 mM	0.3271 mL	1.6355 mL	3.2710 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.18 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.18 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.18 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。