| 常用名 | 达非那新 | CAS号 | 133099-04-4 |
|---|---|---|---|
| 价格 | 纯度 | 97.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情(用途,包装等)
用途: Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.IC50 value: 8.9 (pKi) [1]Target: M3 receptorin vitro: 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].in vivo: 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]. 物理化学性质: CAS号:133099-04-4 常用中文名:达非那新 常用英文名:Darifenacin 分子式:C28H30N2O2 分子量:426.550 密度:1.2±0.1 g/cm3 沸点:614.3±55.0 °C at 760 mmHg 熔点:N/A 闪点:325.3±31.5 °C 储存条件:2-8℃ |