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抑制剂 > 蛋白酵素 > Arecaidine propargyl ester (hydrobromide)
产品名称:
Arecaidine propargyl ester (hydrobromide)
型号:
CS-01Y65235
生产地址
进口、国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

mg 10 mg 25 mg

CAS

116511-28-5

别名

N/A

化学名

N/A

分子式

C10H13NO2·HBr

分子量

260.1

溶解度

DMF: 30 mg/ml,DMSO: 30 mg/ml,PBS (pH 7.2): 10 mg/ml

储存条件

-20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                             

Arecaidine propargyl ester is an agonist of M2 muscarinic acetylcholine receptors (mAChRs).1 It selectively binds to M2 over M1, M3, M4, and M5 mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 µM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2 = 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 µM.2 Arecaidine propargyl ester decreases mean arterial blood pressure in normotensive cats (ED25 = 1.9 nmol/kg).3 It is toxic to house flies (Musca) when administered at a dose of 75 µg/fly.4

1.Scapecchi, S., Matucci, R., Bellucci, C., et al.Highly chiral muscarinic ligands: the discovery of (2S,2’R,3’S,5’R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonistJ. Med. Chem.49(6)1925-1931(2006) 2.Di Bari, M., Tombolillo, B., Conte, C., et al.Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cellsNeurochem. Int.90261-270(2015) 3.Porsius, A.J., and Van Zwieten, P.A.Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of catsProg. Brain Res.47131-135(1977) 4.Honda, H., Tomizawa, M., and Casida, J.E.Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonistsJ. Agric. Food Chem.55(6)2276-2281(2007)

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1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:Arecaidine propargyl ester (hydrobromide) 

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