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Umeclidinium bromide

Umeclidinium bromide

产品编号 T4997   CAS 869113-09-7
别名: 芜地溴铵, GSK573719A

Umeclidinium bromide (GSK573719A) 是mAChR 拮抗剂,作用于克隆的人 M1-M5 mAChRs,Ki 为 0.05 到 0.16 nM。

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Umeclidinium bromide Chemical Structure
Umeclidinium bromide, CAS 869113-09-7
规格 价格/CNY 货期 数量
1 mg ¥ 315 现货
2 mg ¥ 453 现货
5 mg ¥ 728 现货
10 mg ¥ 1,230 现货
25 mg ¥ 2,230 现货
50 mg ¥ 3,730 现货
100 mg ¥ 5,330 现货
1 mL * 10 mM (in DMSO) ¥ 838 现货
产品目录号及名称: Umeclidinium bromide (T4997)
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纯度: 99.09%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Umeclidinium bromide (GSK573719A) is a novel mAChR antagonist.
靶点活性 M5 mAChR:0.13 nM(Ki), M1 mAChR:0.16 nM(Ki), M3 mAChR:0.06 nM(Ki), M4 mAChR:0.05 nM(Ki), M2 mAChR:0.15 nM(Ki)
体外活性 In human embryonic kidney 293 cells, Umeclidinium bromide (GSK573719A) inhibits the human ether-a-go-go-related gene channel tail current in a concentration-dependent manner (IC50=9.4 μM).
体内活性 When Umeclidinium bromide (GSK573719A) is given once daily to mice for 5 consecutive days (0.025 μg intranasally), the level of inhibition on the fifth day is modestly increased above that obtained after a single administration to the same mice (60 versus 35%, respectively). After the fifth day of dosing, the mice are rested for 5 additional days, allowing bronchomotor tone to return to baseline levels. On the sixth day, the mice receive one last dose of antagonist and are once again challenged with Mch. The level of inhibition is essentially the same as that found on the first day of testing, indicating that tolerance is not evident with repeated intranasal delivery of Umeclidinium bromide. On the contrary, when Umeclidinium bromide is given orally (2.0 mg/kg) to mice at a dose 100 times the ED50 value (intranasal), there is no observable protection against an Mch challenge.
动物实验 Mice:Age-matched male BALB/c mice (23-25 gm) are pretreated intranasally (50 μL per mouse) with vehicle (0.9% saline) or Umeclidinium bromide at intervals (0.25-48 hours) prior to methacholine challenge, and placed into individual plethysmograph chambers. Fresh air is supplied by bias flow pumps to the chambers. After baseline respiratory [enhanced pause (Penh)] values are collected, the mice received methacholine (30 mg/mL or EC80) by aerosol delivery (flow=1.6 mL/min×2 minutes). An average Penh is then calculated for 5 minutes. Penh=[(expiratory time/relaxation time)?1]×(peak expiratory flow/peak inspiratory flow), and relaxation time is the amount of time required for 70% of the tidal volume to expire. In some cases, animals are treated on multiple, consecutive days as described in the figure legends. The data are expressed as the mean±S.E.M. percent inhibition of Penh or (mean Penh value of vehicle treated group-Penh for each drug-treated animal) divided by (mean Penh value of vehicle treated group)×100%. Data are analyzed using commercially available software.
别名 芜地溴铵, GSK573719A
分子量 508.49
分子式 C29H34BrNO2
CAS No. 869113-09-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 34 mg/mL (66.86 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9666 mL 9.833 mL 19.6661 mL 49.1652 mL
5 mM 0.3933 mL 1.9666 mL 3.9332 mL 9.833 mL
10 mM 0.1967 mL 0.9833 mL 1.9666 mL 4.9165 mL
20 mM 0.0983 mL 0.4917 mL 0.9833 mL 2.4583 mL
50 mM 0.0393 mL 0.1967 mL 0.3933 mL 0.9833 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Cazzola M, et al. Pharmacology and therapeutics of bronchodilators. Pharmacol Rev. 2012 Jul;64(3):450-504. 2. Calzetta L, et al. Pharmacological characterization of the interaction between umeclidinium and vilanterol in human bronchi. Eur J Pharmacol. 2017 Jul 14. pii: S0014-2999(17)30470-3. 3. Salmon M, et al. Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013 May;345(2):260-70.
Clidinium bromide Pancuronium dibromide Pilocarpine nitrate Promazine hydrochloride Nanofin Metoclopramide hydrochloride VASICINE Leojaponin

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 抗阿尔茨海默症化合物库 GPCR靶点分子库 上市药物库 表型筛选靶点鉴定库 神经信号分子库 药物功能重定位化合物库 NO PAINS 化合物库 经典已知活性库 神经递质受体化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
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每只动物体重
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给药体积
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动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Umeclidinium bromide 869113-09-7 Neuroscience AChR mAChR 芜地溴铵 Umeclidinium Muscarinic acetylcholine receptor inhibit GSK573719A Umeclidinium Bromide Inhibitor inhibitor

 

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