Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Batefenterol (TD-5959) 是一种毒蕈碱受体拮抗剂和β2-肾上腺素受体激动剂,对 hM2、hM3和β2-肾上腺素受体有高亲和力,Ki 值分别为 1.4、1.3 和 3.7 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 568 | 现货 | ||
2 mg | ¥ 791 | 现货 | ||
5 mg | ¥ 1,160 | 现货 | ||
10 mg | ¥ 1,730 | 现货 | ||
25 mg | ¥ 3,290 | 现货 | ||
50 mg | ¥ 4,890 | 现货 | ||
100 mg | ¥ 6,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,890 | 现货 |
产品描述 | Batefenterol (TD-5959) (GSK961081, TD-5959) is a muscarinic receptor antagonist and β2-adrenoceptor agonist. It displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor (Ki:1.4/1.3/3.7 nM). |
靶点活性 | β2:3.7 nM (Ki, cell free), hM3:1.3 nM (Ki, cell free), hM2:1.4 nM (Ki, cell free) |
体外活性 | In competition radioligand binding studies at human recombinant receptors, Batefenterol displays high affinity for hM2 (Ki; 1.4 nM), hM3 muscarinic receptors (Ki: 1.3 nM) and hβ2-adrenoceptors (Ki: 3.7 nM). Batefenterol behaves as a potent hβ2-adrenoceptor agonist (EC50: 0.29 nM for stimulation of cAMP levels) with 440- and 320-fold functional selectivity over hβ1- and hβ3-adrenoceptors, respectively [1]. |
体内活性 | In the guinea pig broncho-protection assay, inhaled Batefenterol produces potent, dose-dependent inhibition of bronchoconstrictor responses via MA (ED50: 33.9 μg/mL), BA (ED50: 14.1 μg/mL), and MABA (ED50: 6.4 μg/mL) mechanisms. Significant bronchoprotective effects of Batefenterol are evident in guinea pigs via MA, BA, and MABA mechanisms for up to 7 days after dosing[1]. In guinea pig isolated trachea expressing native muscarinic M3 and β2, Batefenterol produces smooth muscle relaxation through a dual mechanism involving competitive antagonism of the M3 receptor (EC50: 50 nM) and agonism of the β2 receptor (EC50: 25 nM). The combined effect on both muscarinic receptors and β2 receptors is more potent than either function working alone (EC50: 10 nM) [2]. |
别名 | GSK961081, TD-5959 |
分子量 | 740.24 |
分子式 | C40H42ClN5O7 |
CAS No. | 743461-65-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (135.09 mM)
H2O: < 0.1 mg/mL (insoluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.3509 mL | 6.7546 mL | 13.5091 mL | 33.7728 mL |
5 mM | 0.2702 mL | 1.3509 mL | 2.7018 mL | 6.7546 mL | |
10 mM | 0.1351 mL | 0.6755 mL | 1.3509 mL | 3.3773 mL | |
20 mM | 0.0675 mL | 0.3377 mL | 0.6755 mL | 1.6886 mL | |
50 mM | 0.027 mL | 0.1351 mL | 0.2702 mL | 0.6755 mL | |
100 mM | 0.0135 mL | 0.0675 mL | 0.1351 mL | 0.3377 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。
Batefenterol 743461-65-6 GPCR/G Protein Neuroscience Adrenergic Receptor AChR GSK 961081 mAChR inhibit Muscarinic acetylcholine receptor GSK961081 TD 5959 TD5959 Inhibitor TD-5959 GSK-961081 Beta Receptor inhibitor