Powder: -20°C for 3 years
In solvent: -80°C for 2 years
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 <a href="/target/Fer_FerT_kinase" style="display: inline;">Fer/FerT kinase</a> muscarinic receptor antagonist used to treat urinary incontinence and overactive bladder syndrome. |
| 靶点活性 | M3 mAChR:8.9(pKi) |
| 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] |
| 别名 | UK-88525, 氢溴酸达非那新, Darifenacin HBr |
| 分子量 | 507.472 |
| 分子式 | C28H31BrN2O2 |
| CAS No. | 133099-07-7 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
H2O: <1 mg/mL
DMSO: 93 mg/mL (184 mM)
Ethanol: <1 mg/mL
( < 1 mg/ml refers to the product slightly soluble or insoluble )
参考文献
剂量换算对于不同动物的给药剂量换算，您也可以参考 更多
体内实验配液计算器计算器bottom
您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。
Darifenacin hydrobromide 133099-07-7 Neuroscience AChR 氢溴酸达非那新 UK 88525 Darifenacin UK88525 Muscarinic acetylcholine receptor UK-88525 inhibit mAChR Darifenacin HBr Inhibitor inhibitor
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