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| 5mg |
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| 25mg |
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Purity: ≥98%
Vorapaxar sulfate, the sulfuric acid salt form of Vorapaxar (also known as SCH-530348; Zontivity), is an orally bioactive anti-platelet drug acting as a thrombin receptor protease-activated receptor (PAR-1) antagonist. In 2014, the FDA approved Vorapaxar to help people with poor blood flow or heart attacks avoid having heart attacks and strokes.
| Targets |
PAR-1 ( Ki = 8.1 nM )
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|---|---|
| ln Vitro |
Vorapaxar sulfate (SCH 530348 sulfate) exhibits a strong IC50 of 47 nM for thrombin-induced platelet aggregation and a 25 nM IC50 for haTRAP-induced platelet aggregation. With a Ki of 1.1 nM, vorapaxar sulfate (SCH 530348 sulfate) inhibits the thrombin-induced calcium transient in human coronary artery smooth muscle cells (HCASMC). Additionally, with a Ki of 13 nM, it prevents thrombin-stimulated thymidine incorporation in HCASMC[1].
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| References |
| Molecular Formula |
C29H35FN2O8S
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|---|---|
| Molecular Weight |
590.6602
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| Exact Mass |
590.21
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| Elemental Analysis |
C, 58.97; H, 5.97; F, 3.22; N, 4.74; O, 21.67; S, 5.43
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| CAS # |
705260-08-8
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| Related CAS # |
Vorapaxar; 618385-01-6
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| Appearance |
White to off-white 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.OS(=O)(=O)O
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| InChi Key |
NQRYCIGCIAWEIC-CKLVGUEFSA-N
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| InChi Code |
InChI=1S/C29H33FN2O4.H2O4S/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;1-5(2,3)4/h4-9,12-13,16-17,20,23-27H,3,10-11,14-15H2,1-2H3,(H,32,34);(H2,1,2,3,4)/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;sulfuric acid
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| Synonyms |
SCH-530348; Zontivity; SCH530348; SCH 530348; Vorapaxar sulfate; Vorapaxar
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: ≥ 2.08 mg/mL (3.52 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 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 | 1.6930 mL | 8.4651 mL | 16.9302 mL | |
| 5 mM | 0.3386 mL | 1.6930 mL | 3.3860 mL | |
| 10 mM | 0.1693 mL | 0.8465 mL | 1.6930 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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