常用名 达非那新

英文名 Darifenacin

CAS号 133099-04-4

密度 1.2±0.1 g/cm3

沸点 614.3±55.0 °C at 760 mmHg

分子式 C28H30N2O2

分子量 426.550

闪点 325.3±31.5 °C

精确质量 426.230713

PSA 55.56000

LogP 4.50

蒸汽压 0.0±1.8 mmHg at 25°C

折射率 1.624

储存条件 2-8℃

"Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.

IC50 value: 8.9 (pKi) [1]

Target: M3 receptor

in 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]."

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纯度：99%

配送：惯例下常温**

包装：袋装

厂家：西安齐岳生物科技有限公司

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