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抑制剂 > 神经科学 > Tarafenacin
产品名称:
Tarafenacin
型号:
CS-01Y77128
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

10mg 50mg 100mg

CAS

385367-47-5

别名

 

化学名

[(3R)-1-azabicyclo[2.2.2]octan-3-yl] N-(3-fluorophenyl)-N-[(3,4,5-trifluorophenyl)methyl]carbamate

分子式

C21H20F4N2O2

分子量

408.39

溶解度

Soluble in DMSO

储存条件

Store at -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:                                                                                                            

Tarafenacin is a selective antagonist of M3 muscarinic receptor with Ki value of 0.19nM [1].

Tarafenacin is a novel quinuclidine derivative and is developed as an antimuscarinic drug for treatment of overactive bladder. It shows a 203-fold selectivity with M3 receptor over M2 receptor. Tarafenacin reduces the maximum carbachol response at concentrations of 10nM and 100nM in mouse isolated bladder. In mouse atrial preparations, tarafenacin slightly attenuates the effects on heart rate caused by carbachol. Tarafenacin shows a 199-fold urinary affinity against cardiac affinity. It is a highly potent antagonist in the bladder and lacks any relevant effect in atria at the same range of concentrations. In the guinea pig model, tarafenacin significantly changes the bladder contraction amplitude. It inhibits 25% of spontaneous bladder contractions at dose of 17.1nmol/kg [1].

特别提醒:                                                                                                              

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:Tarafenacin 

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