您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Darifenacin hydrobromide
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Darifenacin hydrobromide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Darifenacin hydrobromide图片
CAS NO:133099-07-7
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Darifenacin HBr
UK-88525
氢溴酸达非那新
产品介绍
Darifenacin HBr 是一种选择性 M3 蕈毒碱受体拮抗剂,pKi 为 8.9。

产品描述

Darifenacin is a selective muscarinic receptor antagonist used to treat urinary incontinence and overactive bladder syndrome.

体外活性

Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat. [1] Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6?μM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6. [2]

体内活性

Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55%. [1] Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers. [3] Darifenacin (7.5 mg and 15 mg, daily) reduces the number of incontinence episodes per week from baseline by 67.7% and 72.8% respectively compared with 55.9% with placebo in patients with overactive bladder (OAB). Darifenacin (7.5 mg and 15 mg, daily) also shows significantly superior to placebo for improvements in micturition frequency, bladder capacity, frequency of urgency, severity of urgency and number of incontinence episodes leading to a change in clothing or pads in patients with overactive bladder (OAB). [4]

Cas No.

133099-07-7

分子式

C28H31BrN2O2

分子量

507.472

别名

Darifenacin HBr;UK-88525;氢溴酸达非那新;Darifenacin hydrobromide

储存和溶解度

DMSO:93 mg/mL (184 mM)
Ethanol:<1 mgml
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years