store at low temperature,keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
2 mg | 在庫あり | ¥ 29,500 |
5 mg | 約 5 days | ¥ 50,000 |
25 mg | 約6-8 週間 | ¥ 158,500 |
50 mg | 約6-8 週間 | ¥ 206,000 |
100 mg | 約6-8 週間 | ¥ 349,000 |
1 mL * 10 mM (in DMSO) | 約 5 days | ¥ 86,000 |
説明 | 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]. |
別名 | SVT-40776 D-tartrate |
分子量 | 558.48 |
分子式 | 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: 80 mg/mL (143.25 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Tarafenacin D-tartrate 1159101-48-0 Neuroscience AChR SVT-40776 D-tartrate Tarafenacin Dtartrate Tarafenacin D tartrate Inhibitor inhibitor inhibit