Vorapaxar
Based on 12 publication(s) in Google Scholar
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
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- Pureté: 99.61%
- CAS No.: 618385-01-6
- Formule: C29H33FN2O4
- Masse moléculaire:492.58
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) Vorapaxar
More- Cell Death Dis. 2020 Jul 9;11(7):520. [Abstract]
- Arterioscler Thromb Vasc Biol. 2023 Feb;43(2):253-266. [Abstract]
- J Med Chem. 2017 Aug 24;60(16):7166-7185. [Abstract]
- J Thromb Haemost. 2023 Aug;21(8):2236-2247. [Abstract]
- Mol Med Rep. 2019 Jun;19(6):5291-5300. [Abstract]
- Neoplasia. 2025 May:63:101153. [Abstract]
- Res Pract Thromb Haemost. 2025 Oct 13;9(7):103223. [Abstract]
- J Cell Biochem. 2023 Sep;124(9):1404-1422. [Abstract]
- Biomed Res Int. 2022 Sep 20;2022:8265898. [Abstract]
- Eur J Oral Sci. 2019 Aug;127(4):287-293. [Abstract]
- Research Square Preprint. 2021 Aug.
- Research Square Preprint. 2021 Mar.
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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WB
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Cell Proliferation/Viability Assay
Activité biologique
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PAR1 8.1 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.064 μM
Compound: SCH530348
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Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
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[PMID: 28745507] |
| Platelet | IC50 |
47 nM
Compound: Zontivity
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Inhibition of thrombin-induced human platelet aggregation
Inhibition of thrombin-induced human platelet aggregation
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[PMID: 38889609] |
Vorapaxar (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. Vorapaxar (SCH 530348) inhibits thrombininduced calcium transient in human coronary artery smooth muscle cells (HCASMC) with a Ki of 1.1 nM. It also inhibits thrombin-stimulated thymidine incorporation in HCASMC with a Ki of 13 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 618385-01-6
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Appearance Solid
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Masse moléculaire 492.58
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Formule C29H33FN2O4
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Color White to off-white
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SMILES
O=C(O[C@@H]1C)[C@@]2([H])[C@]1([H])[C@@H](/C=C/C3=NC=C(C=C3)C4=CC=CC(F)=C4)[C@]([C@](C5)([H])C2)([H])CC[C@H]5NC(OCC)=O
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Synonyms
SCH 530348
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
Twist-mediated PAR1 induction is required for breast cancer progression and metastasis by inhibiting Hippo pathway. [Abstract]2020 Jul 9;11(7):520. PMID: 32647142
Vorapaxar purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Jul 9;11(7):520. [Abstract]
Expression of PAR1, YAP, and TAZ is assessed by Western blotting. Vorapaxar efficiently blocks the expression of YAP and TAZ in T47D-Twist and MDA-MB-231 cells.
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Arterioscler Thromb Vasc Biol
Oligosaccharide Blocks PAR1 (Proteinase-Activated Receptor 1)-PAR4-Mediated Platelet Activation by Binding to Thrombin Exosite II and Impairs Thrombosis. [Abstract]2023 Feb;43(2):253-266. PMID: 36519467 -
J Med Chem
Discovery of Potent Orally Active Protease-Activated Receptor 1 (PAR1) Antagonists Based on Andrographolide. [Abstract]2017 Aug 24;60(16):7166-7185. PMID: 28745507 -
J Thromb Haemost
Protease activated receptors and glycoprotein VI cooperatively drive the platelet component in thromboelastography. [Abstract]2023 Aug;21(8):2236-2247. PMID: 37068592
Vorapaxar purchased from MedChemExpress. Usage Cited in: J Thromb Haemost. 2023 Aug;21(8):2236-2247. [Abstract]
Role of PAR1/PAR4 and Syk in human blood TEG. Healthy volunteer blood samples were analyzed with addition of DMSO (n=4), Vorapaxar (Vora, 5 μM, n=3), BMS-986120 (BMS, 10 μM, n=3) and PRT-2607 (PRT, 20 μM, n=4) to inhibit PAR1, PAR4 and Syk, respectively, 10 mins prior to TEG assay.
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Mol Med Rep
Vorapaxar stabilizes permeability of the endothelial barrier under cholesterol stimulation via the AKT/JNK and NF‑κB signaling pathways. [Abstract]2019 Jun;19(6):5291-5300. PMID: 31059055
Vorapaxar purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Jun;19(6):5291-5300. [Abstract]
Viability rate of endothelial cells following stimulation with different concentrations of Vorapaxar (0-80 μM, 1 h).
Vorapaxar purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Jun;19(6):5291-5300. [Abstract]
Detection of expression levels of p-AKT, AKT, p-JNK, JNK and NF-κB using western blotting. Cells were divided into four groups when cell confluence reached 60–70%, including a control (NC) group, a cholesterol stimulation (CH) group, a cholesterol stimulation with TRAP-6 treatment (CH+T) group and a cholesterol stimulation with vorapaxar treatment (CH+V) group. Cells were treated with TRAP-6 for 5 min and vorapaxar for 1 h before cholesterol stimulation. After being treated with cholesterol for 24 h, cells were washed with sterile PBS to remove extra cholesterol.
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Neoplasia
Targeting PAR1 activation in JAK2V617F-driven philadelphia-negative myeloproliferative neoplasms: Unraveling its role in thrombosis and disease progression. [Abstract]2025 May:63:101153. PMID: 40088673
Vorapaxar purchased from MedChemExpress. Usage Cited in: Neoplasia. 2025 May:63:101153. [Abstract]
The effect of thrombin on PAR1 expression was evaluated, and the inhibitory effect of Vorapaxar on PAR1 expression on the cell surface was tested. To reduce baseline signaling activation before treatments, cells were first serum-starved for 12 h. Following starvation, cells were incubated with Thrombin for 1 h to activate PAR1 expression. For inhibition studies, cells were treated with the PAR1 antagonist Vorapaxar (80 µM) for 10 min before thrombin addition.
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Res Pract Thromb Haemost
Identification of novel gene expression programs in thrombin-stimulated hepatic stellate cells. [Abstract]2025 Oct 13;9(7):103223. PMID: 41278464
Vorapaxar purchased from MedChemExpress. Usage Cited in: Res Pract Thromb Haemost. 2025 Oct 13;9(7):103223. [Abstract]
Immortalized human hepatic stellate cells (LX-2) cells were cultured for 48 hours (48h), then serum starved for 1 hour prior to a 1-hour Fluo4 incubation. Intracellular calcium mobilization was detected by Fluo4 fluorescence in response to thrombin (1 U/mL) or vehicle (Hanks' Balanced Salt Solution) for 2 minutes. Cells were treated with vorapaxar (0.01-10 μM) or vehicle (1% dimethyl sulfoxide in Fluo4 solution) for 1 hour prior to thrombin stimulation. Change in fluorescence relative to baseline following thrombin (or vehicle) stimulation.
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J Cell Biochem
Novel chemical scaffold as potential drug against Leishmania donovani: Integrated computational and experimental approaches. [Abstract]2023 Sep;124(9):1404-1422. PMID: 37566640 -
Biomed Res Int
Hemostatic Effect of 20(S)-Panaxadiol by Induced Platelet Aggregation Depending on Calcium Signaling Pathway. [Abstract]2022 Sep 20;2022:8265898. PMID: 36177062 -
Eur J Oral Sci
Activation of calcium signaling in human gingival fibroblasts by recombinant Porphyromonas gingivalis RgpB protein. [Abstract]2019 Aug;127(4):287-293. PMID: 31175838 -
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Solvant et solubilité
DMSO : 25 mg/mL (50.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (562 KB)
- English - EN (562 KB)
- Français - FR (562 KB)
- Deutsch - DE (562 KB)
- Norwegian - NO (562 KB)
- Español - ES (562 KB)
- Swedish - SV (562 KB)
- Italian - IT (562 KB)
- Korean - KR (562 KB)
- Portuguese - PT (562 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Khoufache K, et al. PAR1 contributes to influenza A virus pathogenicity in mice. J Clin Invest. 2013 Jan;123(1):206-14. [Content Brief]
[2]. Kehinde O, et al. Vorapaxar: A novel agent to be considered in the secondary prevention of myocardial infarction. J Pharm Bioallied Sci. 2016 Apr-Jun;8(2):98-105. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0301 mL | 10.1506 mL | 20.3013 mL | 50.7532 mL |
| 5 mM | 0.4060 mL | 2.0301 mL | 4.0603 mL | 10.1506 mL | |
| 10 mM | 0.2030 mL | 1.0151 mL | 2.0301 mL | 5.0753 mL | |
| 15 mM | 0.1353 mL | 0.6767 mL | 1.3534 mL | 3.3835 mL | |
| 20 mM | 0.1015 mL | 0.5075 mL | 1.0151 mL | 2.5377 mL | |
| 25 mM | 0.0812 mL | 0.4060 mL | 0.8121 mL | 2.0301 mL | |
| 30 mM | 0.0677 mL | 0.3384 mL | 0.6767 mL | 1.6918 mL | |
| 40 mM | 0.0508 mL | 0.2538 mL | 0.5075 mL | 1.2688 mL | |
| 50 mM | 0.0406 mL | 0.2030 mL | 0.4060 mL | 1.0151 mL |
Vorapaxar Related Classifications
HY-10119 Related Classifications
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