Revefenacin (TD-4208)

目录号: GC31761纯度: >98.00%同义词: 雷芬那辛,TD-4208; GSK1160724
Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease.

Revefenacin (TD-4208)
Cas No.: 864750-70-9
规格价格库存数量操作
5mg¥900.00现货
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10mg¥1,620.00现货
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25mg¥2,880.00现货
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50mg¥4,320.00现货
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10mM (in 1mL DMSO)¥1,188.00现货
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产品描述 Description

Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease.

Revefenacin is a high affinity competitive antagonist at human recombinant mAChRs with kinetic functional selectivity for M3 over M2 mAChRs and a potent, slowly reversible antagonist in rat, guinea pig, and human airway tissues expressing native mAChRs[1].

[1] Hegde SS, et al. Pharmacol Res Perspect. 2018, 6(3):e00400.

实验参考方法 Experimental Reference Method

Animal experiment:

Rats: To determine the bronchoprotective and antisialagogue potency after a single dose, rats are exposed by inhalation to a nebulized solution of revefenacin (3–3000 µg/mL), tiotropium (0.3–300 µg/mL), glycopyrronium (1–1000 µg/mL), or vehicle (sterile water). Bronchoprotective activity is assessed 24 hours postdose. For the antisialagogue effect, inhibition of Pilo is assessed 1, 6, or 12 hours after inhalation of an efficacious dose of test compound to determine the time point at which peak effect occurred. All subsequent doses are measured at this time point[2].

References:

[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.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
864750-70-9
同义词
雷芬那辛,TD-4208; GSK1160724
SMILES
O=C(OC1CCN(CCN(C(C2=CC=C(CN3CCC(C(N)=O)CC3)C=C2)=O)C)CC1)NC4=CC=CC=C4C5=CC=CC=C5
分子式
C35H43N5O4
分子量
597.75 g/mol
溶解性
DMSO : ≥ 125 mg/mL (209.12 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

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