货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S82143-5mg	≥99%	￥1640.00 S82143-5mg ￥1640.00 3-5天	0 货期：3-5天	-	-	-	-
S82143-10mg	≥99%	￥2620.00 S82143-10mg ￥2620.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S82143-5mg

≥99%

￥1640.00

货期：3-5天

S82143-10mg

≥99%

￥2620.00

货期：3-5天

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.

靶点：

Others

体外研究：

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

体内研究：

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

参考文献：

1. Salcedo C, et al. In vivo and in vitro pharmacological characterization of SVT-40776, a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder. Br J Pharmacol. 2009 Mar;156(5):807-17. 2. Huang X, et al. Microscopic binding of M5 muscarinic acetylcholine receptor with antagonists by homology modeling, molecular docking, and molecular dynamics simulation. J Phys Chem B. 2012 Jan 12;116(1):532-41.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.791 ml	8.953 ml	17.906 ml
5 mM	0.358 ml	1.791 ml	3.581 ml
10 mM	0.179 ml	0.895 ml	1.791 ml
50 mM	0.036 ml	0.179 ml	0.358 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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浓度

体积

分子摩尔量

计算重置

Tarafenacin (D-tartrate)