2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. Vorapaxar sulfate

Vorapaxar sulfate  (Synonyms: SCH 530348 sulfate)

Cat. No.: HY-10119A Purity: 99.81%
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Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate 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 sulfate Chemical Structure

Vorapaxar sulfate Chemical Structure

CAS No. : 705260-08-8

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5 mg USD 90 In-stock
10 mg USD 150 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
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Based on 11 publication(s) in Google Scholar

Other Forms of Vorapaxar sulfate:

Vorapaxar sulfate Related Antibodies

Top Publications Citing Use of Products

    Vorapaxar sulfate 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.

    View All Protease Activated Receptor (PAR) Isoform Specific Products:

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    PAR1 PAR2 PAR4

    • Biological Activity

    • Purity & Documentation

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    Description

    Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner[1].

    IC50 & Target

    PAR1

    8.1 nM (Ki)

    In Vitro

    Vorapaxar sulfate (SCH 530348 sulfate) 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 sulfate (SCH 530348 sulfate) 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.

    Vorapaxar sulfate Related Antibodies
    Clinical Trial
    Molecular Weight

    590.66

    Formula

    C29H35FN2O8S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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.O=S(O)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (211.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (3.52 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.52 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation
    References

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6930 mL 8.4651 mL 16.9302 mL 42.3255 mL
    5 mM 0.3386 mL 1.6930 mL 3.3860 mL 8.4651 mL
    10 mM 0.1693 mL 0.8465 mL 1.6930 mL 4.2326 mL
    15 mM 0.1129 mL 0.5643 mL 1.1287 mL 2.8217 mL
    20 mM 0.0847 mL 0.4233 mL 0.8465 mL 2.1163 mL
    25 mM 0.0677 mL 0.3386 mL 0.6772 mL 1.6930 mL
    30 mM 0.0564 mL 0.2822 mL 0.5643 mL 1.4109 mL
    40 mM 0.0423 mL 0.2116 mL 0.4233 mL 1.0581 mL
    50 mM 0.0339 mL 0.1693 mL 0.3386 mL 0.8465 mL
    60 mM 0.0282 mL 0.1411 mL 0.2822 mL 0.7054 mL
    80 mM 0.0212 mL 0.1058 mL 0.2116 mL 0.5291 mL
    100 mM 0.0169 mL 0.0847 mL 0.1693 mL 0.4233 mL
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    Vorapaxar sulfate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Vorapaxar705260-08-8SCH 530348SCH530348SCH-530348Protease Activated Receptor (PAR)Thrombin receptorsInhibitorinhibitorinhibit

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