store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tarafenacin D-tartrate is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over the M2 receptor.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 977 | 现货 | ||
5 mg | ¥ 1,650 | 5日内发货 | ||
25 mg | ¥ 5,340 | 6-8周 | ||
50 mg | ¥ 6,940 | 6-8周 | ||
100 mg | ¥ 11,700 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,890 | 5日内发货 |
产品描述 | Tarafenacin D-tartrate is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over the M2 receptor. |
体外活性 | Tarafenacin D-tartrate is highly selective for M(3) over M(2) receptors (Ki = 0.19 nmol.L(-1) for M(3) receptor affinity). Tarafenacin D-tartrate was the most potent in inhibiting carbachol-induced bladder contractions of the anticholinergic agents tested, without affecting atrial contractions over the same range of concentrations. Tarafenacin D-tartrate exhibited the highest urinary versus cardiac selectivity (199-fold). Tarafenacin D-tartrate has a much higher binding affinity (K(d) = 0.4 nM) to M5 mAChR than that of solifenacin (K(d) = 31 nM) with the same receptor. The calculated binding free energy change (-2.3 ± 0.3 kcal/mol) from solifenacin to Tarafenacin D-tartrate is in good agreement with the experimentally derived binding free energy change (-2.58 kcal/mol), suggesting that our modeled M5 mAChR structure and its complexes with the antagonists are reliable [1][2]. |
体内活性 | Tarafenacin D-tartrate inhibited 25% of spontaneous bladder contractions at a very low dose (6.97 microg.kg(-1) i.v) in the guinea pig in vivo model, without affecting arterial blood pressure [1]. |
别名 | SVT-40776 D-tartrate |
分子量 | 558.48 |
分子式 | C25H26F4N2O8 |
CAS No. | 1159101-48-0 |
store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (179.06 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7906 mL | 8.9529 mL | 17.9057 mL | 44.7644 mL |
5 mM | 0.3581 mL | 1.7906 mL | 3.5811 mL | 8.9529 mL | |
10 mM | 0.1791 mL | 0.8953 mL | 1.7906 mL | 4.4764 mL | |
20 mM | 0.0895 mL | 0.4476 mL | 0.8953 mL | 2.2382 mL | |
50 mM | 0.0358 mL | 0.1791 mL | 0.3581 mL | 0.8953 mL | |
100 mM | 0.0179 mL | 0.0895 mL | 0.1791 mL | 0.4476 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。
Tarafenacin D-tartrate 1159101-48-0 Others Tarafenacin Dtartrate SVT-40776 D-tartrate Tarafenacin D tartrate Inhibitor inhibitor inhibit