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Tarafenacin

CAT: 0804-HY-14825Size: 1 EachDry Ice: NoHazardous: No
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Description
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 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].
CAS Number
385367-47-5
Product Name Alternative
SVT-40776
UNSPSC
12352005
Target
MAChR
Type
Reference compound
Related Pathways
GPCR/G Protein; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/tarafenacin.html
Solubility
10 mM in DMSO
Smiles
O=C(O[C@H]1CN2CCC1CC2)N(C3=CC=CC(F)=C3)CC4=CC(F)=C(F)C(F)=C4
Molecular Formula
C21H20F4N2O2
Molecular Weight
408.39
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
MAChR3

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B1132-100Tarafenacin
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GTR19153651-01Tarafenacin (SVT-40776)
MBS386586-01SVT-40776 (Tarafenacin)
A21477-100Tarafenacin D-tartrate 100mg
A10808-5SVT-40776 (Tarafenacin) 5mg
A21477-50Tarafenacin D-tartrate 50mg
A21477-25Tarafenacin D-tartrate 25mg
A21477-10Tarafenacin D-tartrate 10mg
A21477-5Tarafenacin D-tartrate 5mg

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