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SVT-40776

更新时间:2024-07-15 12:30:19 采购访问:14次

常用名 Tarafenacin D-酒石酸盐 CAS号 1159101-48-0
价格 纯度 99.0%
备货期 10天 库存 现货
 产品详情(用途,包装等)
用途:
Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.IC50 value: 0.19 nM (Ki) [1]Target: M3 muscarinic receptorin vitro: SVT-40776 is highly selective for M(3) over M(2) receptors (Ki = 0.19 nmol.L(-1) for M(3) receptor affinity). SVT-40776 was the most potent in inhibiting carbachol-induced bladder contractions of the anti-cholinergic agents tested, without affecting atrial contractions over the same range of concentrations. SVT-40776 exhibited the highest urinary versus cardiac selectivity (199-fold) [1]. SVT-40776 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 reeptor. The calculated binding free energy change (-2.3 ± 0.3 kcal/mol) from solifenacin to SVT-40776 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 [2].in vivo: In the guinea pig in vivo model, SVT-40776 inhibited 25% of spontaneous bladder contractions at a very low dose (6.97 microg.kg(-1) i.v), without affecting arterial blood pressure [1].
物理化学性质:
CAS号:1159101-48-0
常用中文名:Tarafenacin D-酒石酸盐
常用英文名:Tarafenacin (D-tartrate)
分子式:C25H26F4N2O8
分子量:558.47600
密度:N/A
沸点:N/A
熔点:N/A
闪点:N/A
储存条件:2-8℃

供应商信息

上海念兴实业有限公司 认证供应商

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联系人电话:0086-021-52280163
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参考价格:$451/10mM*1mLinDMSO
其他供应商价格:
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