store at low temperature,keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tarafenacin D-tartrate is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over the M2 receptor.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 127.00 | |
5 mg | 5 days | $ 217.00 | |
25 mg | 6-8 weeks | $ 690.00 | |
50 mg | 6-8 weeks | $ 897.00 | |
100 mg | 6-8 weeks | $ 1,520.00 | |
1 mL * 10 mM (in DMSO) | 5 days | $ 373.00 |
Description | Tarafenacin D-tartrate is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over the M2 receptor. |
In vitro | Tarafenacin D-tartrate is highly selective for M(3) over M(2) receptors (Ki = 0.19 nmol.L(-1) for M(3) receptor affinity). Tarafenacin D-tartrate 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. Tarafenacin D-tartrate exhibited the highest urinary versus cardiac selectivity (199-fold). Tarafenacin D-tartrate 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 Tarafenacin D-tartrate 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]. |
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 |
store at low temperature,keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (179.06 mM)
You can also refer to dose conversion for different animals. More
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Tarafenacin D-tartrate 1159101-48-0 Others Tarafenacin Dtartrate SVT-40776 D-tartrate Tarafenacin D tartrate inhibitor inhibit