1. Vitamin D Related/Nuclear Receptor
  2. Androgen Receptor
  3. BMS-564929

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。

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BMS-564929 Chemical Structure

BMS-564929 Chemical Structure

CAS No. : 627530-84-1

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10 mM * 1 mL in DMSO ¥1540
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1 mg ¥636
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5 mg ¥1400
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10 mg ¥2300
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50 mg ¥9300
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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)[1]

体外研究
(In Vitro)

BMS-564929 在 C2C12 成肌细胞系中表现出 0.44±0.03 nM 的效力 (EC50,计算为达到 DHT 最大刺激作用的 50% 时的浓度)。在PEC细胞系中,BMS-564929 的 EC50 为 8.66±0.22 nM。BMS-564929 对 AR 的选择性是雌激素受体 (ER) α 和 β、糖皮质激素受体 (GR) 和盐皮质激素受体 (MR) 的 1000 多倍,是孕激素受体 (PR) 的约 400 倍。在浓度高达 30 μM 时,BMS-564929 在 ERα/β、GR、MR 或 PR 的功能反式激活测定中未显示出可测量的活性[1]

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

体内研究
(In Vivo)

在性成熟、阉割的雄性大鼠中,BMS-564929 (po) 在提肛肌中表现出明显更有效的活性,在提肌中的 ED50 为 0.0009 mg/kg 和 在前列腺中的 ED50 为 0.14 mg/kg;肌肉与前列腺的选择性净高 160 倍。在 0.1 mg/kg 时达到大约 100% 的肌肉刺激,在 0.3 和 1 mg/kg 时达到大于 125% 的刺激。与同一模型中的丙酸 T (TP) 相比,BMS-564929 对肌肉的刺激作用强 200 多倍,对肌肉和前列腺的选择性强 80 倍[1]

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

分子量

305.72

Formula

C14H12ClN3O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (163.55 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.18 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    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。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 98.17%

参考文献
Kinase Assay
[1]

The human cancer epithelial breast cell lines MDA MB-453 and T47D, which endogenously express AR and progesterone receptor (PR), respectively, are used for radioligand competition binding assays. Binding assays are conducted by incubating BMS-564929 at various concentrations with either [3H]DHT or [3H]progesterone with the cells for 2 h at room temperature. For ERα and ERβ, fusion proteins expressed in Escherichia coli, consisting of maltose binding protein, a specific biotinylation sequence, an enterokinase cleavage site, and either the ERα or ERβ LBD is used. Binding reactions are conducted by incubating ERα and ERβ LBD with BMS-564929 and [3H]E2 for 2 h at room temperature. Specific binding activity to the mineralocorticoid receptor (MR) by BMS-564929 is evaluated by competition binding assay using kidney cytosolic preparations and [3H]aldosterone. The kidneys are obtained from adrenalectomized rats to remove the endogenous source of aldosterone and to increase the MR concentration in the cytosol of kidney cells. Binding reactions are incubated for 2 h on ice in the presence of excess mifepristone (RU486) to block nonspecific glucocorticoid receptor (GR) binding. A fluorescence polarization based assay is used for GR binding, as per manufacturer recommendations. Inhibitory constants (Ki, app) defining apparent binding affinity of test compounds to intracellular receptors are calculated from the observed inhibition of natural ligand binding at multiple concentrations of test compound. SHBG binding is performed using a standard charcoal assay. Reagents: 1 mg lyophilized SHGB powder (Tris), [3H]DHT, 3% charcoal, and 0.4% Dextran in PBS; binding buffer: 50 mM Tris, pH 7.6, 100 mM NaCl, 1 mM EDTA, 1 mM DTT, and mock lysate (3.5 μg/100 μL buffer); stock solutions: stock SHBG protein: 1 mg/mL in water=20 μM; stock [3H]DHT ligand: 9 μM; DHT: 10 mM in DMSO; BMS 564929: 10 mM in DMSO. Compounds diluted in binding buffer are added to 40 nM [3H]DHT and 20 nM SHBG protein in 200 μL volume and incubated for 1 h at room temperature. Total binding: 40 nM [3H]DHT and 20 nM SHBG protein in 200 μL volume; nonspecific binding: 40 nM [3H]DHT and 20 nM SHBG protein and 1 mM cold DHT in 200 μL volume. At the end of the incubation period, 200 μL of the charcoal solution (3% containing 0.04% dextran) is added to 200 μL of the reactions and shaken for 15 min before centrifugation. Supernatant (200 μL) is then transferred to the wells of a 24-well white Optiplate; 200 μL of scintillant are added with mixing. Radioactivity counts are read in Topcount[1].

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

Animal Administration
[1]

Rats[1]
Matched sets of castrated, sexually mature Harlan Sprague Dawley rats (42-56 d old, 200-250 g) are dosed once daily by oral gavage with BMS-564929 (0.00001-10 mg/kg) in solution/suspension of 80% PEG 400 and 20% Tween 20 for 14 d. Two control groups, one sham operated intact and one castrated, are dosed orally with the PEG/TW vehicle only, beginning on d 15 after surgery. Animals are dosed (vol/wt) at 1 mL/kg body weight. T propionate (TP) is dosed once daily sc in a 10% ethanol/90% peanut oil vehicle as a reference compound (0.03-10 mg/kg). After 14 d of treatment, the animals are killed by carbon dioxide asphyxiation, the levator ani and the ventral prostate are surgically removed and weighed, and serum is collected for LH measurements.

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

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2710 mL 16.3548 mL 32.7097 mL 81.7742 mL
5 mM 0.6542 mL 3.2710 mL 6.5419 mL 16.3548 mL
10 mM 0.3271 mL 1.6355 mL 3.2710 mL 8.1774 mL
15 mM 0.2181 mL 1.0903 mL 2.1806 mL 5.4516 mL
20 mM 0.1635 mL 0.8177 mL 1.6355 mL 4.0887 mL
25 mM 0.1308 mL 0.6542 mL 1.3084 mL 3.2710 mL
30 mM 0.1090 mL 0.5452 mL 1.0903 mL 2.7258 mL
40 mM 0.0818 mL 0.4089 mL 0.8177 mL 2.0444 mL
50 mM 0.0654 mL 0.3271 mL 0.6542 mL 1.6355 mL
60 mM 0.0545 mL 0.2726 mL 0.5452 mL 1.3629 mL
80 mM 0.0409 mL 0.2044 mL 0.4089 mL 1.0222 mL
100 mM 0.0327 mL 0.1635 mL 0.3271 mL 0.8177 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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