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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). |
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靶点：
Protease-activated Receptor;Protease-activatedReceptor |
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. |
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溶解性：
H2O:<1 mg/mL Ethanol:92 mg/mL (186.8 mM) DMSO:92 mg/mL (186.8 mM) |
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保存条件：
2-8℃ |
配置溶液浓度参考：
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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 |
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| 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。 |
上海工商
北京