Mepenzolate bromide (Synonyms:溴美喷酯;溴化甲哌佐酯)
目录号 : KM18002 CAS No. : 76-90-4 纯度 : 98%

Mepenzolate bromide 是一种有效的,具有口服活性的毒蕈碱受体拮抗剂,对 hM2R 和 hM3R 的 Ki 分别为 0.68 和 2.6 nM。Mepenzolate bromide 可用于抑制与肠易激综合征相关的胃肠道过度运动。Mepenzolate bromide 是一种 GPR109A 抑制剂.

规格 价格 是否有货 数量
100mg
In-stock
500mg
In-stock
1g 询价 In-stock
5g 询价 In-stock

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生物活性

Mepenzolate bromide is an orally administered muscarinic receptor antagonist with Kis of 0.68 and 2.6 nM for hM2R and hM3R, respectively. Mepenzolate bromide can be used to suppress the gastrointestinal hypermotility associated with irritable bowel syndrome.Mepenzolate bromide is a GPR109A inhibitor.

体外研究

Mepenzolate not only exerts an anti-inflammatory effect via a muscarinic receptor-independent mechanism, but also a bronchodilatory effect via a muscarinic receptor-dependent mechanism. Mepenzolate is a subtype-non-specific muscarinic antagonist whose bronchodilatory effect and inhibitory effect on intestinal motility can be explained by its antagonistic action on M3R.

体内研究

Mepenzolate bromide, a GPR109A receptor blocker, abolishes the beneficial effects of niacin on body weight, colon wet weight as well as colonic levels of myeloperoxidase (MPO) and VEGF. 
Mepenzolate bromide is a muscarinic antagonist. Intratracheal administration or inhalation of Mepenzolate bromide decreases the severity of elastase-induced airspace enlargement and respiratory dysfunction. Mepenzolate bromide may be an effective therapeutic for the treatment of chronic obstructive pulmonary disease (COPD) due to its anti-inflammatory and bronchodilatory activities.

Animal Model: Adult male Wistar rats, weighing 150-200 g
Dosage: 5  mg/kg
Administration: Intraperitoneal injection
Result: Abolished the protective effect of niacin against iodoacetamide-induced rise in colon wet weight as well as the colonic levels of both MPO and VEGF.
Animal Model: ICR mice (4-6 weeks old, male) and DBA/2 mice (5 weeks old, female)
Dosage: 0.04, 0.38, 3.8, 38 μg/kg; 45.2 and 226 μg per chamber
Administration: "0.04, 0.38, 3.8, 38 μg/kg administered intratracheally once daily for 14 days
45.2 and 226 μg per chamber by inhalation once daily for 14 days"
Result: The simultaneous daily intratracheal administration suppressed this enlargement in a dose-dependent manner.
The inhalation route was similar to those observed with the intratracheal mode of administration.
分子式
C21H26BrNO3
分子量
420.34
CAS号
76-90-4
中文名称
溴美喷酯;溴化甲哌佐酯
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 : ≥ 35 mg/mL (83.27 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 2.3790 mL 11.8951 mL 23.7903 mL
5 mM 0.4758 mL 2.3790 mL 4.7581 mL
10 mM 0.2379 mL 1.1895 mL 2.3790 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。

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The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
动物实验计算换算器
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系客服为您提供正确的澄清溶液配方)
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计算结果:

工作液浓度 mg/ml;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积

1. 首先保证母液是澄清的;
           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。