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• 产品描述： Darifenacin is a selective muscarinic receptor antagonist used to treat urinary incontinence and overactive bladder syndrome.

• 靶点： AChR

• 体内研究：
  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%. 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. 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).

• 参考文献：
  1.Hegde SS, et al. Br J Pharmacol, 1997, 120(8), 1409-1418. 2.Haab F, et al. Eur Urol, 2004, 45(4), 420-429. 3.Miller DW, et al. Neurourol Urodyn, 2011, 30(8), 1633-1638. 4.Iijima K, et al. Eur Urol, 2007, 52(3), 842-847.

• 溶解性： Ethanol:<1  mg/mL    H2O:<1  mg/mL    DMSO:93  mg/mL  (184  mM)

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.971 ml	9.853 ml	19.706 ml
  5 mM	0.394 ml	1.971 ml	3.941 ml
  10 mM	0.197 ml	0.985 ml	1.971 ml
  50 mM	0.039 ml	0.197 ml	0.394 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *