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首页-小分子抑制剂&激动剂-GPCR-mAChR-Umeclidinium bromide
Umeclidinium bromide

Chemical Structure : Umeclidinium bromide

CAS No.: 869113-09-7

Umeclidinium bromide (GSK573719A, GSK573719A)

货号: PC-42894Not For Human Use, Lab Use Only.

Umeclidinium bromide (GSK573719A) is potent, long-acting, inhaled antagonist of mAChRs with Ki of 0.05-0.16 nM for human M1-M5 mAChRs.

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50 mg ¥2180 In stock
100 mg ¥3580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Umeclidinium bromide (GSK573719A) is potent, long-acting, inhaled antagonist of mAChRs with Ki of 0.05-0.16 nM for human M1-M5 mAChRs.
Umeclidinium bromide demonstrates picomolar potency (-log pA2=23.9 pM) in an acetylcholine-mediated Ca(2+) mobilization assay in CHO cells transfected M3 mAChRs.
Umeclidinium bromide dose dependently blocks Ach-induced bronchoconstriction with long duration of action in mice model of pulmonary diseases.

物理化学性质&存储条件

分子量 508.4897
分子式 C29H34BrNO2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 34 mg/mL

Chemical Name/SMILES

1-Azoniabicyclo[2.2.2]octane, 4-(hydroxydiphenylmethyl)-1-[2-(phenylmethoxy)ethyl]-, bromide (1:1)

参考文献

1. Salmon M, et al. J Pharmacol Exp Ther. 2013 May;345(2):260-70.

2. Tal-Singer R, et al. Eur J Pharmacol. 2013 Feb 15;701(1-3):40-8.

3. Decramer M, et al. Respir Physiol Neurobiol. 2013 Jan 15;185(2):393-9.

4. Decramer M, et al. Lancet Respir Med. 2014 Jun;2(6):472-86.

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