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• 产品描述： Vorapaxar (SCH 530348) is an effective and orally active thrombin receptor (PAR-1) antagonist (Ki: 8.1 nM).

• 靶点： Protease-activated Receptor

• 体内研究： SCH 530348 is well absorbed in rat (68%; 10 mg/kg) and in monkey (82%; 1 mg/kg) models. Tmax is observed at about 3 h in rats and 1 h in monkeys. The elimination half-life is 5.1 h in rats and 13 h in monkeys. The oral bioavailability is 33% in rats and 86% in monkeys. In preclinical studies in cynomolgus monkey platelets, oral administration of SCH 530348 at a dose greater than 0.1 mg/kg resulted in 100% inhibition of thrombin-receptor agonist peptide (TRAP)-induced platelet aggregation for 24 h with partial recovery occurring at 48 h.

• 参考文献：
  1.Chackalamannil S, et al. J Med Chem, 2008, 51(11), 3061-3064. 2.Tang W, Huang B, Wang J, et al. A label-free screening approach targeted protease-activated receptor 1 based on dynamic mass redistribution in living cells[J]. RSC Advances. 2017, 7(68): 43005-43013.

• 溶解性： H2O:<1  mg/mL    Ethanol:92  mg/mL  (186.8  mM)    DMSO:92  mg/mL  (186.8  mM)

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.03 ml	10.151 ml	20.301 ml
  5 mM	0.406 ml	2.03 ml	4.06 ml
  10 mM	0.203 ml	1.015 ml	2.03 ml
  50 mM	0.041 ml	0.203 ml	0.406 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。

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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 分子量 (g/mol)

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