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Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a selective and potent muscarinic acetylcholine M3 receptor antagonist used in the study of overactive bladder and bronchial disorders.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $127 | In Stock | |
5 mg | $217 | 5 days | |
25 mg | $690 | 6-8 weeks | |
50 mg | $897 | 6-8 weeks | |
100 mg | $1,520 | 6-8 weeks | |
1 mL x 10 mM (in DMSO) | $373 | 5 days |
Description | Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a selective and potent muscarinic acetylcholine M3 receptor antagonist used in the study of overactive bladder and bronchial disorders. |
In vitro | D-tartrate Tarafenacin was more selective for M(3) receptors than for M(2) receptors (Ki = 0.19 nmol.L(-1) for M(3) receptor affinity). Of the anticholinergic drugs tested, tarafenacin tartrate had the strongest inhibitory effect on carbachol-induced bladder contraction but did not affect atrial contraction over the same concentration range. Tarafenacin D-tartrate had the highest selectivity (199-fold) for urine and heart.The binding affinity of tarafenacin D-tartrate for the M5 mAChR (K(d) = 0.4 nM) was much higher than that of solifenacin (K(d) = 31 nM) for the same receptor.The binding affinity of tarafenacin D-tartrate for the M5 mAChR was much higher than that for solifenacin (K(d) = 31 nM). The calculated change in free energy of binding from solifenacin to tarafenacin tartrate (-2.3 ± 0.3 kcal/mol) agrees well with the experimentally derived change in free energy of binding (-2.58 kcal/mol), suggesting that our modeled structure of the M5 mAChR and its complex with the antagonist is reliable [1][2]. |
In vivo | Tarafenacin D-tartrate 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]. |
Alias | SVT-40776 D-tartrate |
Molecular Weight | 558.48 |
Formula | C25H26F4N2O8 |
Cas No. | 1159101-48-0 |
Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (143.25 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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