Tarafenacin

Name: Tarafenacin
Brand: TargetMol
SKU: T16990
Rating: 4.5 (1 reviews)

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产品编号 T16990Cas号 385367-47-5

别名 SVT-40776

Tarafenacin is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over the M2 receptor.

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产品编号 T16990 别名 SVT-40776Cas号 385367-47-5

Tarafenacin is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over the M2 receptor.

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产品描述	Tarafenacin is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over the M2 receptor.
体外活性	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 anticholinergic 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 receptor. 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 [1][2].
体内活性	SVT-40776 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