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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $127 | - | In Stock | |
| 5 mg | $217 | 5 days | 5 days | |
| 25 mg | $690 | 6-8 weeks | 6-8 weeks | |
| 50 mg | $897 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $1,520 | 6-8 weeks | 6-8 weeks | |
| 1 mL x 10 mM (in DMSO) | $373 | 5 days | 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]. |
| Synonyms | SVT-40776 D-tartrate |
| Molecular Weight | 558.48 |
| Formula | C25H26F4N2O8 |
| Cas No. | 1159101-48-0 |
| Smiles | 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 |
| Relative Density. | no data available |
| Color | White |
| Appearance | Solid |
| 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/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (143.25 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.91 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
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DMSO
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