• 提示：详情请下载说明书。

• 产品描述： Tasimelteon (BMS 214778, VEC 162) is a selective dual melatonin receptor (MT1/MT2) agonist with 2.1-4.4 times greater affinity for the MT2 receptor believed to mediate circadian rhythm phase-shifting (Ki = 0.0692 nM and Ki = 0.17 nM in NIH-3T3 and CHOeK1 cells, respectively), than for the MT1 receptor (Ki = 0.304 nM and Ki = 0.35 nM, respectively).

• 靶点： MT2 receptor:9.8(pKi);MT1 receptor:9.45(pKi)

• 体内研究： In rats and monkeys, the half-life of tasimelteon was approximately 2 h which is longer than the half-life of melatonin. Tasimelteon has a mean absolute bioavailability of approximately 38.3%. The higher oral-to-IV exposure ratios and decrease in the metabolite-to-parent ratios after IV administration for tasimelteon's metabolites indicate that although tasimelteon is subject to first-pass metabolism, a substantial fraction of its metabolism occurs post- rather than presystemically. Both oral and IV tasimelteon were well tolerated

• 参考文献：
  1. Lankford DA. Expert Opin Investig Drugs. 2011, 20(7):987-93. 2. Torres R1, et al. Am J Ther. 2015, 22(5):355-60. 3. Rosarelis Torres, et al. J Clin Pharmacol. 2015, 55(5): 525–533.

• 溶解性： Soluble  in  DMSO

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	4.076 ml	20.382 ml	40.763 ml
  5 mM	0.815 ml	4.076 ml	8.153 ml
  10 mM	0.408 ml	2.038 ml	4.076 ml
  50 mM	0.082 ml	0.408 ml	0.815 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

输入产品批号：

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 分子量 (g/mol)

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