Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Mirabegron (YM178) 是选择性的肾上腺素受体激动剂,EC50=22.4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 279 | 现货 | ||
2 mg | ¥ 397 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 1,160 | 现货 | ||
25 mg | ¥ 2,170 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 5,390 | 现货 | ||
500 mg | ¥ 10,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 728 | 现货 |
产品描述 | Mirabegron (YM178) is a beta-3 adrenergic agonist that is used for treatment of overactive bladder syndrome. |
靶点活性 | β3-adrenoceptor:22.4 nM(EC50) |
体外活性 | 在麻醉大鼠中,静脉注射Mirabegron(3 mg / kg)能够产生降低节律性膀胱收缩频率,但不会影响收缩幅度. |
体内活性 | 在表达人类3-肾上腺素能受体CHO细胞中,Mirabegron以浓度依赖的方式增加cAMP在细胞内的积累。在用10-6M或10-7M卡巴胆碱预处理的大鼠膀胱平滑肌(EC50=5.1 μM)和人膀胱平滑肌(EC50=0.78 μM)中,Mirabegron能够产生放松作用。 |
细胞实验 | Mirabegron (YM178) is dissolved in 100% DMSO and diluted with assay buffer[1]. CHO cells (105) are seeded in each well of a 24-well culture plate and subcultured. Three days later, the medium is exchanged with 250 μL/well Hanks' balanced salt solution containing 0.1 mM 3-isobutyl-1-methylxanthine, pH 7.4. The cells are incubated with each compound (isoproterenol, Mirabegron, BRL37344, and CL316,243 at final concentrations of 10-10 to 10-4 M) for 10 min at 37°C, after which incubation is stopped by the addition of 250 μL of 0.2 M HCl. cAMP concentration in the reaction mixture is measured by radioimmunoassay using an 125I-cAMP assay system using a gamma counter. Fifty microliters of reaction mixture is incubated with 50 μL of succinyl agent for 10 min at room temperature, after which the reaction is stopped by the addition of 400 μL of buffer solution. Fifty microliters of succinylated sample is incubated with 50 μL of 125I-cAMP and 50 μL of anti-cAMP antibody for 24 h at 4°C. At the end of the incubation period, 250 μL of charcoal suspension is added and centrifuged for 10 min at 2800 g at 4°C. Two hundred and fifty microliters of supernatant is transferred into a tube and counted for 1 min using a gamma counter. The intrinsic activity (I.A.) relative to isoproterenol for each β-adrenoceptor agonist is calculated using the maximal response of each compound[1]. |
别名 | YM178, 米拉贝隆 |
分子量 | 396.51 |
分子式 | C21H24N4O2S |
CAS No. | 223673-61-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 8 mg/mL (20.17 mM)
DMSO: 73 mg/mL (184.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.522 mL | 12.61 mL | 25.22 mL | 63.0501 mL |
5 mM | 0.5044 mL | 2.522 mL | 5.044 mL | 12.61 mL | |
10 mM | 0.2522 mL | 1.261 mL | 2.522 mL | 6.305 mL | |
20 mM | 0.1261 mL | 0.6305 mL | 1.261 mL | 3.1525 mL | |
DMSO | 50 mM | 0.0504 mL | 0.2522 mL | 0.5044 mL | 1.261 mL |
100 mM | 0.0252 mL | 0.1261 mL | 0.2522 mL | 0.6305 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Mirabegron 223673-61-8 GPCR/G Protein Neuroscience Adrenergic Receptor Inhibitor cAMP CHO YM 178 YM-178 YM178 米拉贝隆 inhibit Beta Receptor inhibitor