| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Vorapaxar (formerly SCH-530348; SCH530348; Zontivity), a new anti-platelet drug based on the natural product himbacine, is a thrombin receptor protease-activated receptor (PAR-1) antagonist that inhibits thrombin-induced platelet activation. In order to lower the risk of thrombotic cardiovascular events, vorapaxar, a platelet aggregation inhibitor, was approved in 2014. For those with poor blood flow or who have already experienced a heart attack, it can prevent heart attacks and strokes. Unlike other anti-platelet drugs like aspirin and P2Y12 inhibitors, vorapaxar works by preventing thrombin-related platelet aggregation.
| Targets |
PAR-1 ( Ki = 8.1 nM )
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|---|---|
| ln Vitro |
SCH 530348 is an orally administered thrombin-receptor antagonist based on himbacine and a synthetic tricyclic 3-phenylpyridine. SCH 530348 exhibits no inhibition of platelet aggregation induced by other agonists such as ADP, collagen, and a PAR-4 agonist peptide, but it exhibits strong inhibition of thrombin-induced platelet aggregation (IC50 of 47 nM) and haTRAP-induced platelet aggregation (IC50 of 25 nM). Additionally, prothrombin time (PT), partial thromboplastin time (PTT), and activated partial thromboplastin time (aPTT) are unaffected by SCH 530348. Furthermore, when SCH 530348 is used in place of an inactive control, there is no increase in bleeding time or surgical bleeding. When SCH530348 is tested against several ion channels and receptors, including the PAR-4 receptor, it is discovered to be selective for PAR-1.[1]
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| ln Vivo |
SCH 530348 is well absorbed in rat (68%; 10 mg/kg) and in monkey (82%; 1 mg/kg) models. In rats, Tmax is measured at approximately 3 hours, while in monkeys, it is measured at 1 hour. In rats, the elimination half-life is 5.1 hours, while in monkeys, it is 13 hours. In rats, the oral bioavailability is 33%, while in monkeys, it is 86%. Oral SCH 530348 administration at a dose greater than 0.1 mg/kg resulted in 100% inhibition of thrombin-receptor agonist peptide (TRAP)-induced platelet aggregation for 24 hours, with partial recovery taking place at 48 hours, according to preclinical studies conducted on platelets from cynomolgus monkeys.[1]
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| Enzyme Assay |
From 40 units of fresh human platelets, 700 mg of human platelet membranes are made. A thrombin receptor radioligand binding assay modification is used to screen for thrombin receptor antagonists. Human platelet membranes (40μg) are incubated in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA) with 10nM of [3H]haTRAP (alanine-p-fluorophenylalaninearganine-cyclohexylalanine-homoarganine-[3H]phenylalanine amide) in the presence of compounds at concentrations of 1 nM, 3 nM, 30 nM, 100 nM, 300 nM, and 1μM (5% DMSO final concentration). The plates are placed on a plate shaker, covered, and gently vortexed for one hour at room temperature. Using a Packard FilterMate Universal Harvester, the incubated membranes are harvested onto Packard UniFilter GF/C filter plates. These plates are soaked in 0.1% polyethyleneimine for at least an hour and then quickly washed four times with 300 μL of ice cold binding buffer without BSA. Each well receives an addition of MicroScint 20 scintillation cocktail, and the plates are counted using a Packard TopCount Microplate Scintillation Counter. In the presence of excess (50 μM) unlabeled haTRAP, the specific binding is defined as the total binding minus the nonspecific binding.
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| Animal Protocol |
cynomolgus monkeys
0.5, 0.3, 0.1, and 0.05 mg/kg oral |
| References |
| Molecular Formula |
C29H33FN2O4
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|---|---|
| Molecular Weight |
492.5817
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| Exact Mass |
492.24
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| Elemental Analysis |
C, 70.71; H, 6.75; F, 3.86; N, 5.69; O, 12.99
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| CAS # |
618385-01-6
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| Related CAS # |
Vorapaxar sulfate; 705260-08-8
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| Appearance |
Solid powder
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| 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
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| InChi Key |
ZBGXUVOIWDMMJE-QHNZEKIYSA-N
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| InChi Code |
InChI=1S/C29H33FN2O4/c1-3-35-29(34)32-23-10-11-24-20(14-23)15-26-27(17(2)36-28(26)33)25(24)12-9-22-8-7-19(16-31-22)18-5-4-6-21(30)13-18/h4-9,12-13,16-17,20,23-27H,3,10-11,14-15H2,1-2H3,(H,32,34)/b12-9+/t17-,20+,23-,24-,25+,26-,27+/m1/s1
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| 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
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| Synonyms |
Vorapaxar free base; Vorapaxar; SCH530348; SCH-530348; SCH 530348
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25~99 mg/mL (50.8~201 mM)
Ethanol: ~99 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5%DMSO + 40%PEG300 + 5%Tween 80 + 50%ddH2O: 1.67mg/ml (3.39mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0301 mL | 10.1506 mL | 20.3013 mL | |
| 5 mM | 0.4060 mL | 2.0301 mL | 4.0603 mL | |
| 10 mM | 0.2030 mL | 1.0151 mL | 2.0301 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03207451 | Completed | Drug: Vorapaxar and Aspirin Drug: Vorapaxar |
Coronary Artery Disease Myocardial Infarction |
Inova Health Care Services | January 1, 2016 | Phase 4 |
| NCT02875028 | Completed | Drug: Vorapaxar Drug: Placebo |
Healthy Volunteers | Medical University of Vienna | June 2016 | Phase 4 |
| NCT02475837 | Completed | Drug: Vorapaxar sulfate Drug: Placebo |
AV Fistula | Ken Mahaffey | August 26, 2015 | Phase 2 |
| NCT02394730 | Completed | Drug: vorapaxar Drug: Placebo |
HIV | Kirby Institute | September 2015 | Phase 1 Phase 2 |
| NCT02545933 | Completed | Drug: Vorapaxar Drug: Prasugrel |
Myocardial Infarction | University of Florida | February 2016 | Phase 4 |
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