Vorapaxar sulfate (Synonyms: SCH 530348 sulfate)
目录号: PL10689 纯度: ≥99%
CAS No. :705260-08-8
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中文名称
Vorapaxar sulfate
中文别名
硫酸沃拉帕沙;SCH 530348 (H2SO4 Salt) 沃拉帕沙;Vorapaxar硫酸盐;硫酸沃拉帕沙杂质;沃拉帕沙;沃拉帕沙硫酸盐
英文名称
Vorapaxar sulfate
英文别名
SCH 530348 (H2SO4 Salt);Vorapaxar Sulfate;ethyl N-[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethenyl]-1-methyl-3-oxo-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-1H-benzo[f][2]benzofuran-6-yl]carbamate,sulfuric acid;Vorapaxar-D5
Cas No.
705260-08-8
分子式
C29H33N2O4F.H2O4S
分子量
590.66
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Vorapaxar sulfate (SCH 530348 sulfate),抗血小板药物,是一种选择性、口服活性和竞争性的凝血酶受体蛋白酶激活受体 (PAR-1) 拮抗剂,Ki 值为 8.1 nM。Vorapaxar sulfate剂量依赖性抑制凝血酶受体激活肽 (TRAP) 诱导的血小板聚集。
生物活性
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (K i =8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
性状
Solid
IC50 & Target[1][2]
Ki: 8.1 nM (PAR-1)
体外研究(In Vitro)
Vorapaxar sulfate (SCH 530348 sulfate) shows potent inhibition of thrombin-induced platelet aggregation with an IC50 of 47 nM and haTRAP-induced platelet aggregation with an IC50 of 25 nM. Vorapaxar sulfate (SCH 530348 sulfate) inhibits thrombininduced calcium transient in human coronary artery smooth muscle cells (HCASMC) with a Ki of 1.1 nM. It also inhibits thrombin-stimulated thymidine incorporation in HCASMC with a Ki of 13 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Khoufache K, et al. PAR1 contributes to influenza A virus pathogenicity in mice. J Clin Invest. 2013 Jan;123(1):206-14.
[2]. Kehinde O, et al. Vorapaxar: A novel agent to be considered in the secondary prevention of myocardial infarction. J Pharm Bioallied Sci. 2016 Apr-Jun;8(2):98-105.
溶解度数据
In Vitro: DMSO : 125 mg/mL (211.63 mM; Need ultrasonic)H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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