Tarafenacin (D-tartrate) [CAS 1159101-48-0]
Tarafenacin (D-tartrate) [CAS 1159101-48-0]
SKU:QM-0149630-01
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Product Details
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Description
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) [1] 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) [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].
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CAS Number
[1159101-48-0]
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Molecular Formula
C25H26F4N2O8
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Molecular Weight
558.48
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Smiles
O=C(O[C@H]1CN2CCC1CC2)N(C3=CC=CC(F)=C3)CC4=CC(F)=C(F)C(F)=C4.O[C@@H]([C@@H](C(O)=O)O)C(O)=O
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Target
MAChR
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Isoform
MAChR3
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Concentration
10mM
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Purity
99.86
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Solubility
DMSO : ≥ 100 mg/mL
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Storage Conditions
4°C (Powder, sealed storage, away from moisture)
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Shipping Conditions
Room Temperature
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Tarafenacin (D-tartrate) [CAS 1159101-48-0]
Tarafenacin (D-tartrate) is a premium-grade research compound supplied by Quantimol for laboratory and scientific applications.