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.
| 生物活性 | Mepenzolate bromide is an orally administeredmuscarinic receptorantagonist withKis of 0.68 and 2.6 nM forhM2RandhM3R, respectively. Mepenzolate bromide can be used to suppress the gastrointestinal hypermotility associated with irritable bowel syndrome[1].Mepenzolate bromide is aGPR109Ainhibitor[2]. |
| IC50& Target | |
体外研究
(In Vitro) | 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[1].
|
体内研究
(In Vivo) | 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[2].
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[3].
| Animal Model: | Adult male Wistar rats, weighing 150-200 g[2] | | 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)[3] | | 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. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 35 mg/mL(83.27 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.95 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.95 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.95 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com