| 品牌 | 货号 | 产品规格 | 价格(RMB) | 库存（上海） | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
| 源叶(MedMol) | S86846-1mg | 99% | ￥200.00元 | 9 | - | - | - |
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| 源叶(MedMol) | S86846-5mg | 99% | ￥410.00元 | >10 | - | - | - |
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| 源叶(MedMol) | S86846-10mg | 99% | ￥750.00元 | >10 | - | - | - |
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| 源叶(MedMol) | S86846-100mg | 99% | ￥2200.00元 | 8 | - | - | - |
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| 产品描述： Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM | ||||||||||||||||||||
| 靶点： Ki: 0.42 nM (M1), 0.32 nM (M2), 0.18 nM (M3), 0.56 nM (M4), 6.7 nM (M5);AChR | ||||||||||||||||||||
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体外研究： The Kis of revefenacin are 0.42, 0.32, 0.18, 0.56, and 6.7 nM at human M1, M2, M3, M4 and M5 receptors, respectively. In a functional assay, revefenacin is shown to be a functional antagonist with inhibition constants similar to binding Ki's. Revefenacin also inhibits agonist-induced contraction of guinea pig isolated tracheal ring preparation with an affinity of 0.1 nM, similar to the measured M3 biding Ki |
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体内研究： In anesthetized dogs, revefenacin, along with tiotropium and glycopyrronium, produce sustained inhibition of acetylcholine-induced bronchoconstriction for up to 24 hours. In anesthetized rats, inhaled revefenacin exhibits dose-dependent 24-hour bronchoprotection against methacholine-induced bronchoconstriction. The estimated 24-hour potency is 45.0 µg/mL and the bronchoprotective potencies are maintained after 7 days of once-daily dosing |
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参考文献： 1. Steinfeld T, et al. In vitro characterization of TD-4208, a lung-selective and long-acting muscarinic antagonist bronchodilator (Abstract). Am J Respir Crit Care Med 179:A4553. 2. Pulido-Rios MT, et al. In vivo pharmacological characterization of TD-4208, a novel lung-selective inhaled muscarinic antagonist with sustained bronchoprotective effect in experimental animal models. J Pharmacol Exp Ther. 2013 Aug;346(2):241-50. |
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| 溶解性： soluble in DMSO | ||||||||||||||||||||
| 保存条件： -20℃ | ||||||||||||||||||||
配置溶液浓度参考：
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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