| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
| S81503-1mg | 99% | ￥240.00 | 3 | - | - | - |
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| S81503-5mg | 99% | ￥400.00 | 2 | - | - | - |
|
| S81503-10mg | 99% | ￥530.00 | 1 | - | - | - |
|
| S81503-25mg | 99% | ￥970.00 | 2 | - | - | - |
|
| S81503-50mg | 99% | ￥1680.00 | 货期：2-3天 | - | - | - |
|
Vorapaxar (SCH 530348) is an effective and orally active thrombin receptor (PAR-1) antagonist (Ki: 8.1 nM).
| 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. | ||||||||||||||||||||
| 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： |
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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。 |
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