品牌：源叶(MedMol)

产品编号：S81503 一键复制产品信息

CAS号：618385-01-6

分子式：C₂₉H₃₃FN₂O₄

分子量：492.5817232

别名：维拉帕莎;沃拉帕沙工艺,中间体及其杂质;维拉帕莎,沃拉帕沙;Vorapaxar;Vorapaxar (SCH 530348);[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(1E)-2-[5-(3-Fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1-methyl-3-oxonaphtho[2,3-c]furan-6-yl]-carbami

货号	规格	价格	上海	北京	武汉	南京
S81503-1mg	99.8%	￥240.00 S81503-1mg ￥240.00 现货	3 3	-	-	-
S81503-5mg	99.8%	￥400.00 S81503-5mg ￥400.00 现货	1 1	-	-	-
S81503-10mg	99.8%	￥530.00 S81503-10mg ￥530.00 现货	1 1	-	-	-
S81503-25mg	99.8%	￥970.00 S81503-25mg ￥970.00 现货	2 2	-	-	-
S81503-50mg	≥99%	￥1680.00 S81503-50mg ￥1680.00 2-3天	0 货期：2-3天	-	-	-

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产品介绍

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).

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：

	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。

参考文献

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