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溴美喷酯 /Mepenzolate bromide {[allProObj[0].p_purity_real_show]}

货号:A288808 同义名: Mepenzolate (bromide);NSC 4358

Mepenzolate bromide mAchR antagonist, working as a post-ganglionic parasympathetic inhibitor to decrease gastric acid and pepsin secretion and suppresse spontaneous contractions of the colon.

Mepenzolate bromide 化学结构 CAS号:76-90-4
Mepenzolate bromide 化学结构
CAS号:76-90-4
Mepenzolate bromide 3D分子结构
CAS号:76-90-4
Mepenzolate bromide 化学结构 CAS号:76-90-4
Mepenzolate bromide 3D分子结构 CAS号:76-90-4
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Mepenzolate bromide 纯度/质量文件 产品仅供科研

货号:A288808 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AChE AChR mAChR nAChR 其他靶点 纯度
Donepezil +++

hAChE, IC50: 11.6 nM

bAChE, IC50: 8.12 nM

98%
Loganin ++

AChE, IC50: 3.95 μM

99%+
topride HCl ++

AChE, IC50: 2.04 μM

98%
Dehydroevodiamine HCl 99%+
Jatrorrhizine ++

AChE, IC50: 872 nM

99%+
Palmatine ++

AChE, IC50: 0.51 μM

98%
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

98%
Galanthamine HBr ++

AChE, IC50: 0.35 μM

98%
Trospium chloride 99%
Tiotropium Bromide Monohydrate 98+%
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

98%
Hexamethonium Bromide 99%
Pancuronium dibromide 98%
Neostigmine bromide 98%
Orphenadrine citrate 98%
Oxybutynin 98%
Irsogladine PDE 98%
Pyridostigmine bromide 99+%
Rivastigmine +

AChR, IC50: 5.5 μM

98%
Paroxetine hydrochloride 97%
Rocuronium Bromide 98%
Tropicamide +++

M4 mAChR, IC50: 8 nM

98%
Diphenmanil methylsulfate 98%
Umeclidinium bromide 95%
Otilonium bromide 98%
Flavoxate HCl +

mAChR, IC50: 12.2 μM

98%
Ipratropium bromide 98%
Diphenidol HCl 98%
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

98%
Aclidinium Bromide ++++

M4 mAChR, Ki: 0.21 nM

M2 mAChR, Ki: 0.1 nM

98%
Oxybutynin chloride 99%
Pentoxyverine citrate 98%
Solifenacin 98%
Catharanthine 98%
Benzethonium chloride +++

α7 nAChRs, IC50: 122 nM

α4β2 nAChRs, IC50: 49 nM

99+%
Vinblastine sulfate +

nAChR, IC50: 8.9 μM

99%
PNU-120596 ++

α7 nAChR, EC50: 216 nM

99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Mepenzolate bromide 生物活性

描述 Mepenzolate bromide (MP), an antagonist for human muscarinic M3 receptor (hM3R), has both anti-inflammatory and short-acting bronchodilatory activities[3]. Mepenzolate bromide, used to treat gastrointestinal disorders in clinical settings, also displayed beneficial effects in chronic obstructive pulmonary disease and pulmonary fibrosis of a mouse model by inhibiting inflammatory responses and reducing oxidative stress[4]. Apart from suppressing elastase-induced pulmonary inflammatory responses and the production of superoxide anions, mepenzolate bromide reduces the level of cigarette smoke-induced airspace enlargement and respiratory dysfunction. Mpenzolate bromide may be an effective therapeutic for the treatment of COPD (chronic obstructive pulmonary disease) due to its anti-inflammatory and bronchodilatory activities[5]. The intratracheal administration of mepenzolate reduced bleomycin-induced pulmonary fibrosis and lung dysfunction in mice[6].

Mepenzolate bromide 参考文献

[1]Tanaka K, Kurotsu S, et al. Superiority of pulmonary administration of mepenzolate bromide over other routes as treatment for chronic obstructive pulmonary disease. Sci Rep. 2014 Mar 28;4:4510.

[2]Tanaka K, Ishihara T, et al. Mepenzolate bromide displays beneficial effects in a mouse model of chronic obstructive pulmonary disease. Nat Commun. 2013;4:2686.

[3]Tanaka KI, Yamakawa N, Yamashita Y, et al. Identification of Mepenzolate Derivatives With Long-Acting Bronchodilatory Activity. Front Pharmacol. 2018;9:344. Published 2018 Apr 10

[4]Zheng Y, Wang X, Ji S, et al. Mepenzolate bromide promotes diabetic wound healing by modulating inflammation and oxidative stress. Am J Transl Res. 2016;8(6):2738‐2747. Published 2016 Jun 15

[5]Tanaka K, Ishihara T, Sugizaki T, et al. Mepenzolate bromide displays beneficial effects in a mouse model of chronic obstructive pulmonary disease. Nat Commun. 2013;4:2686

[6]Kurotsu S, Tanaka K, Niino T, et al. Ameliorative effect of mepenzolate bromide against pulmonary fibrosis. J Pharmacol Exp Ther. 2014;350(1):79‐88

Mepenzolate bromide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.90mL

2.38mL

1.19mL

23.79mL

4.76mL

2.38mL

Mepenzolate bromide 技术信息

CAS号76-90-4
分子式C21H26BrNO3
分子量 420.34
别名 Mepenzolate (bromide);NSC 4358;mepenzolic acid;mepenzolate iodide;Cantilon;Cantilaque;Gastropidil;Cantil
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 250 mg/mL(594.76 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 10 mg/mL(23.79 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方
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