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Revefenacin

(Synonyms: TD-4208; GSK1160724)

目录号: PL06849 纯度: ≥99%

Revefenacin (TD-4208;GSK1160724) 是有效的 mAChR 拮抗剂，在M3受体上具有高亲和力，Ki 值为0.18 nM。

CAS No. :864750-70-9

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中文名称	Revefenacin
中文别名	Revefenacin
英文名称	Revefenacin
英文别名	TD-4208;1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-N-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate;Revefenacin;Yupelri;GSK1160724;G2AE2VE07O;[1-[2-[[4-[(4-carbamoylpiperidin-1-yl)methyl]benzoyl]-methylamino]ethyl]piperidin-4-yl] N-(2-phenylphenyl)carbamate;1-(2-(4-((4-Carbamoylpiperidin-1-yl)methyl)-N-methylbenzamido)ethyl)piperidin-4-yl N-((1,1'-biphenyl)-2-yl)carbamate;Revefenacin [INN
Cas No.	864750-70-9
分子式	C₃₅H₄₃N₅O₄
分子量	597.75
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	Revefenacin (TD-4208;GSK1160724) 是有效的 mAChR 拮抗剂，在M3受体上具有高亲和力，Ki 值为0.18 nM。

产品详情

Revefenacin (TD-4208;GSK1160724) 是有效的 mAChR 拮抗剂，在M3受体上具有高亲和力，K_i 值为0.18 nM。

生物活性

Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a K i of 0.18 nM.

性状

Solid

IC50 & Target[1][2]

Ki: 0.42 nM (M1), 0.32 nM (M2), 0.18 nM (M3), 0.56 nM (M4), 6.7 nM (M5)

体外研究(In Vitro)

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 Kis. 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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (167.29 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Revefenacin

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