Tarafenacin D-tartrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tarafenacin D-tartrate (SVT-40776 D-tartrate) 是高亲和性M3毒蕈碱受体选择性拮抗剂，Ki为0.19 nM，比对M2受体的亲和性高200倍。

Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.IC50 value: 0.19 nM (Ki) Target: M3 muscarinic receptor in 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) . 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 .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 .

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Cell Cycle/DNA Damage

AChR

AChR

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1159101-48-0

558.48

C25H26F4N2O8

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 100 mg/mL (179.06 mM )

O[C@@H]([C@H](O)C(O)=O)C(O)=O.Fc1cccc(c1)N(Cc1cc(F)c(F)c(F)c1)C(=O)O[C@H]1CN2CCC1CC2

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(-20℃)

With Ice Pack

≥ 2 years