计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
沃拉帕沙, PAR1 拮抗剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Information
Vorapaxar (MK-5348) Vorapaxar (SCH 530348, MK-5348) is a potent and orally active thrombin receptor (PAR-1) antagonist with K i of 8.1 nM.
In vitro
SCH 530348 is a synthetic tricyclic 3-phenylpyridine and an orally active himbacine-based thrombin-receptor antagonist. SCH 530348 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, whereas it shows no inhibition of platelet aggregation induced by other agonists such as ADP, collagen and a PAR-4 agonist peptide. SCH 530348 also has no affect on the prothrombin time (PT), partial thromboplastin time (PTT), or activated partial thromboplastin time (aPTT). Moreover, SCH 530348 causes no increase in the bleeding time or in surgical bleeding compared with inactive control. SCH530348 is found to be selective for PAR-1 when tested over a number of ion channels and receptors, including PAR-4 receptor.
In vivo
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.
Cell Data
cell lines：JVM13
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
英文别名
SCH 530348 | Carbamic acid, N-[(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]-, ethyl ester
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Vorapaxar (MK-5348)
生化机理
Vorapaxar（SCH 530348，MK-5348）是一种强效口服活性凝血酶受体（PAR-1）拮抗剂，其Ki值为 8.1 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
作用机制
PAR1 拮抗剂
名称和识别符
EC号
612-523-7
分子类型
小分子
Isomeric SMILES
CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]3[C@H]([C@H]2/C=C/C4=NC=C(C=C4)C5=CC(=CC=C5)F)[C@H](OC3=O)C
PubChem CID
分子量
492.58
技术文档
高级数据
产品属性
| ALogP | 5.261 |
|---|---|
| HBD Count | 1 |
| Rotatable Bond | 6 |
关联靶点（人）
F2R
Tclin
蛋白酶激活受体 1(Proteinase-activated receptor 1)
(13 活性数据)
化学和物理性质
DMSO(mg / mL) Max Solubility
99
DMSO(mM) Max Solubility
200.9825815
Water(mg / mL) Max Solubility
＜1
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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