Vorapaxar sulfate
(Synonyms: 硫酸沃拉帕沙,SCH 530348 sulfate) 目录号 : GC64347
A PAR1 antagonist
Cas No.:705260-08-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Vorapaxar is an orally bioavailable competitive antagonist of the proteinase-activated receptor (PAR1; Ki = 8.1 nM), also known as the thrombin receptor.1 It is selective for PAR1 over other PARs, as well as a number of GPCRs, ion channels, and receptors. It inhibits platelet aggregation induced by thrombin and haTRAP (IC50s = 47 and 25 nM, respectively). Vorapaxar (0.1 mg/kg, i.v.) completely inhibits platelet aggregation in cynomolgus monkeys ex vivo. Formulations containing vorapaxar are used in the prevention of thrombotic cardiovascular events.
1.Chackalamannil, S., Wang, Y., Greenlee, W.J., et al.Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activityJ. Med. Chem.51(110)3061-3064(2008)
| Cas No. | 705260-08-8 | SDF | Download SDF |
| 别名 | 硫酸沃拉帕沙,SCH 530348 sulfate | ||
| 分子式 | C29H35FN2O8S | 分子量 | 590.66 |
| 溶解度 | DMSO : 125 mg/mL (211.63 mM; Need ultrasonic)|Water : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) | 储存条件 | 4°C, away from moisture |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.693 mL | 8.4651 mL | 16.9302 mL |
| 5 mM | 0.3386 mL | 1.693 mL | 3.386 mL |
| 10 mM | 0.1693 mL | 0.8465 mL | 1.693 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Vorapaxar for reduction of thrombotic cardiovascular events in myocardial infarction and peripheral artery disease
Am J Health Syst Pharm 2015 Oct 1;72(19):1615-22.PMID:26386102DOI:10.2146/ajhp140758.
Purpose: The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, dosage and administration, cost, and place in therapy of vorapaxar in the secondary prevention of atherosclerotic events are reviewed. Summary: Vorapaxar is a highly selective, reversible antagonist of protease-activated receptor-1 expressed on platelets. Vorapaxar competitively inhibits thrombin from activating the receptor, thereby decreasing platelet aggregation. Vorapaxar is rapidly absorbed and distributed, with peak plasma levels being reached within 60-90 minutes. Vorapaxar's effective half-life is three to four days and its terminal elimination half-life is eight days. Vorapaxar sulfate 2.5 mg (equivalent to 2.08 mg of vorapaxar) orally daily without a loading dose was clinically effective for the secondary prevention of ischemic events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease (PAD) without a history of stroke. Phase II and III trials of vorapaxar given with aspirin or a thienopyridine or both demonstrated a reduction in the primary endpoint of cardiovascular death, MI, and stroke in patients with a history of MI or coronary artery disease and PAD. Patients with a history of stroke were found to have an increased rate of intracranial hemorrhage (ICH), which led to a boxed warning placed on vorapaxar's labeling to warn of the increased risk for bleeding in patients with a history of stroke. Conclusion: Vorapaxar is a novel antiplatelet agent that has demonstrated efficacy in reducing atherosclerotic events in patients with a history of MI or PAD without a history of stroke, transient ischemic attack, or ICH when taken in combination with aspirin and clopidogrel.
Vorapaxar, a Protease-Activated Receptor-1 Antagonist, a Double-Edged Sword!
Recent Adv Cardiovasc Drug Discov 2014;9(2):73-7.PMID:26104312DOI:10.2174/1574890110666150624100815.
Acute coronary syndrome (ACS) constitutes a group of pathophysiological entities resulting from reduced blood flow in the coronary arteries leading to decreased or improper functioning or death of heart muscle. Such patients are usually prescribed combination antiplatelet drug therapy, containing acetylsalicylic acid (aspirin) and an adenosine diphosphate receptor inhibitor to prevent recurrence of ischemic events. The combination prophylactic therapy to certain extend has been successful in preventing secondary complications including ischemic/thrombotic events in these patients. However, research is still on for newer advances in anti-thrombotic therapy that can further prevent secondary complications of Acute Coronary Syndrome. Vorapaxar is a newer drug recommended along with aspirin or clopidogril for prevention of recurrence of cardiac events. Vorapaxar, a thrombin receptor antagonist acts by reversible inhibition of the protease-activated receptor-1 (PAR-1). PAR-1 is expressed on platelets, and it inhibits platelet aggregation, both thrombin-induced and thrombin receptor agonist peptide (TRAP)-induced. Various trials world -wide have documented its efficacy as an anti-platelet agent for preventing recurrent cardiovascular ischemic events but at the expense of increased bleeding complications including intracranial haemorrhage (ICH), when compared to standard therapy alone. For the same reason, vorapaxar is contraindicated in patients with prior stroke, transient ischemic attack and ICH. U.S. Food and Drug Administration (FDA) approved vorapaxar in May 2014 as an antiplatelet agent along with standard anti-platelet therapy for the reduction of recurring thrombotic cardiovascular events in patients with a history of myocardial infarction or with peripheral arterial disease. Vorapaxar is developed and marketed by Merck Sharp Dohme and is available by the brand name 'Zontivity' as 2.5 mg oral tablet equivalent to 2.08 mg of Vorapaxar sulfate. There are two patents protecting this drug.