Vorapaxar
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Vorapaxar是一种有效的PAR1抑制剂和抗血小板药物，已完成III期临床试验[1]。
PAR1是4种凝血酶受体中的一种，属于G蛋白偶联受体超家族[1]。通过结合凝血酶，血小板表面PAR1的N端精氨酸41和丝氨酸42位点之间的键可被酶促反应切断，导致血小板及后续止血过程的激活[1]。
Vorapaxar是一种由天然himbacine衍生的乙基氨基甲酸酯分子，是一种可直接结合的选择性PAR 1抑制剂[2]。在充满血小板的人类血浆中，Vorapaxar可抑制血小板聚集，IC50值为47 nM[2]。此外，vorapaxar可抑制凝血酶受体激活肽增加引起的血小板聚集，IC50值为25 nM[2]。同时，vorapaxar不能抑制添加9,11-双脱氧-11R,9R-环氧乙烷前列腺素F2R（一种血栓素模拟物）导致的血小板聚集，证明其并不干扰凝血酶对纤维形成或血栓素A2受体诱导的血小板聚集的酶催化活性[1]。
在体内，口服0.1 mg/kg的Vorapaxar 24小时可在猴模型中完全抑制血小板聚集。在26,449位病人的III期临床试验[1]中，相比安慰剂组，服用vorapaxar（2.5 mg/天）可减少统计上显著的1.2%的心血管死亡或缺血性事件的发生率[1]。
参考文献：
[1]. Chackalamannil S & XIA, Y. Thrombin receptor (PAR-1) antagonists as novel antithrombotic agents. Expert Opinion on Therapeutic Patents, 2006.16:493-505.
[2]. Chackalamannil S, Wang Y, Greenlee W J et al. 2008. Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J Med Chem, 2008,51: 3061-3064.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 492.58 |
| Cas No. | 618385-01-6 |
| Formula | C29H33FN2O4 |
| Solubility | ≥24.65 mg/mL in DMSO; insoluble in H2O; ≥10.64 mg/mL in EtOH with ultrasonic |
| Chemical Name | 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 |
| SDF | Download SDF |
| Canonical SMILES | CCOC(=O)NC1CCC2C(C1)CC3C(C2C=CC4=NC=C(C=C4)C5=CC(=CC=C5)F)C(OC3=O)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | Vorapaxar（SCH 530348）是一种有效的具有口服活性的凝血酶受体（PAR-1）拮抗剂，Ki值为8.1 nM。 | |||||
| 靶点 | PAR-1 | |||||
| IC50 | 8.1 nM (Ki) | |||||
质量控制和MSDS
- 批次:
化学结构
