Umeclidinium bromide - CAS:869113-09-7

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Umeclidinium bromide (Synonyms:芜地溴铵; GSK573719A)

目录号 : KM2809 CAS No. : 869113-09-7 纯度 : 98%

Data Sheet 产品使用指南

Umeclidinium bromide 是一种 mAChR 拮抗剂。Umeclidinium bromide 作用于克隆的人 M1-M5 mAChRs，K_i 为 0.05 到 0.16 nM。

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生物活性

Umeclidinium bromide is a novel mAChR antagonist. The affinity (K_i) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.

体外研究

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). Umeclidinium bromide, previously known as GSK573719, is a novel high-affinity specific mAChR antagonist. It is a potent agent that demonstrates slow functional reversibility at cloned human M₃ mAChRs and at endogenous mAChR in isolated human bronchus.

体内研究

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. By contrast, 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.

分子式

C₂₉H₃₄BrNO₂

分子量

508.49

CAS号

869113-09-7

中文名称

芜地溴铵；芜地溴氨；芜地溴胺

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
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 25 mg/mL (49.17 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9666 mL	9.8330 mL	19.6661 mL
5 mM	0.3933 mL	1.9666 mL	3.9332 mL
10 mM	0.1967 mL	0.9833 mL	1.9666 mL

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO→90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (4.92 mM); Clear solution; Need ultrasonic

此⽅案可获得 2.5 mg/mL (4.92 mM) 的澄清溶液

以 1 mL ⼯作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀。
2.

请依序添加每种溶剂： 10% DMSO→90% corn oil

Solubility: 2.5 mg/mL (4.92 mM); Suspended solution; Need ultrasonic

此⽅案可获得 2.5 mg/mL (4.92 mM) 的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射

以 1 mL ⼯作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ⽟⽶油中，混合均匀。