1. GPCR/G Protein
  2. Protease-Activated Receptor (PAR)
  3. Vorapaxar

Vorapaxar (Synonyms: SCH 530348)

Cat. No.: HY-10119 Purity: 99.91%
Handling Instructions

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.

For research use only. We do not sell to patients.

Vorapaxar Chemical Structure

Vorapaxar Chemical Structure

CAS No. : 618385-01-6

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 185 In-stock
Estimated Time of Arrival: December 31
5 mg USD 168 In-stock
Estimated Time of Arrival: December 31
10 mg USD 288 In-stock
Estimated Time of Arrival: December 31
25 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 900 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Vorapaxar:

Top Publications Citing Use of Products

    Vorapaxar purchased from MCE. Usage Cited in: Cell Death Dis. 2020 Jul 9;11(7):520.

    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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1].

    IC50 & Target

    Ki: 8.1 nM (PAR-1)[1]

    In Vitro

    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].

    Clinical Trial
    Molecular Weight

    492.58

    Formula

    C₂₉H₃₃FN₂O₄

    CAS No.

    618385-01-6

    SMILES

    O=C(O[[email protected]@H]1C)[[email protected]@]2([H])[[email protected]]1([H])[[email protected]@H](/C=C/C3=NC=C(C=C3)C4=CC=CC(F)=C4)[[email protected]]([[email protected]](C5)([H])C2)([H])CC[[email protected]]5NC(OCC)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 150 mg/mL (304.52 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      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

    • 2.

      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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.91%

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    Keywords:

    VorapaxarSCH 530348SCH530348SCH-530348Protease-Activated Receptor (PAR)Thrombin receptorsInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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