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

Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.

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

CAS No. : 423735-93-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Parmodulin 2 purchased from MedChemExpress. Usage Cited in: Nat Cardiovasc Res. 2025 Aug;4(8):964-975.  [Abstract]

    Western blot for phospho-PKC (P-PKC) and actin in lysates of Human Lung Microvascular Lymphatic Endothelial Cells (HMVEC-LLy) grown in culture and treated with 1 unit/ml thrombin for 10 min +/- pretreatment with 10 μM parmodulin2 (PM2) for 1 hour.

    Parmodulin 2 purchased from MedChemExpress. Usage Cited in: Nat Cardiovasc Res. 2025 Aug;4(8):964-975.  [Abstract]

    Representative IVIS images of ICG fluorescence detected over the chest of mice after intratracheal ICG instillation, demonstrating the retention of ICG in Parmodulin 2 (PM2) (10 mg/kg)-treated mice.

    Parmodulin 2 purchased from MedChemExpress. Usage Cited in: Kidney360. 2024 Jan 1;5(1):8-21.  [Abstract]

    Representative sections of αSMA immunolabeling in Parmodulin (125 μg/500 μL)-treated or PBS-treated mice 49 days after CA/CPR.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM[1]. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo[2].

    IC50 & Target[1]

    PAR1

    .26 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HepG2 CC50
    > 150 μM
    Compound: 1; ML161
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability
    [PMID: 31320211]
    In Vitro

    Parmodulin 2 (ML161; 10 μM; for 30 minutes) inhibits proinflammatory signaling in endothelial HUVECs cells[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Parmodulin 2 (ML161; 5 mg/kg; IV) significantly inhibits platelet thrombus formation, with a 73% inhibition in AUC (area under the curve)[2].
    Parmodulin 2 inhibits platelet thrombus formation in vivo, and it does not prolong bleeding time. Parmodulin 2 selectively inhibits platelet aggregation through Par1 and the α2A-adrenergic receptor[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: C57BL/6J wild type mice[2]
    Dosage: 5 mg/kg (Pharmacokinetic Analysis)
    Administration: IV
    Result: Significantly inhibited platelet thrombus formation, with a 73% inhibition in AUC.
    Molecular Weight

    361.23

    Formula

    C17H17BrN2O2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC=CC(NC(CCC)=O)=C1)C2=CC=CC=C2Br

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 100 mg/mL (276.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7683 mL 13.8416 mL 27.6832 mL
    5 mM 0.5537 mL 2.7683 mL 5.5366 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, 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.92 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.
    • Protocol 2

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

      Solubility: 2.5 mg/mL (6.92 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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

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    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    %
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    %
    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).
    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

    Purity: 99.82%

    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, 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 2.7683 mL 13.8416 mL 27.6832 mL 69.2080 mL
    5 mM 0.5537 mL 2.7683 mL 5.5366 mL 13.8416 mL
    10 mM 0.2768 mL 1.3842 mL 2.7683 mL 6.9208 mL
    15 mM 0.1846 mL 0.9228 mL 1.8455 mL 4.6139 mL
    20 mM 0.1384 mL 0.6921 mL 1.3842 mL 3.4604 mL
    25 mM 0.1107 mL 0.5537 mL 1.1073 mL 2.7683 mL
    30 mM 0.0923 mL 0.4614 mL 0.9228 mL 2.3069 mL
    40 mM 0.0692 mL 0.3460 mL 0.6921 mL 1.7302 mL
    50 mM 0.0554 mL 0.2768 mL 0.5537 mL 1.3842 mL
    60 mM 0.0461 mL 0.2307 mL 0.4614 mL 1.1535 mL
    80 mM 0.0346 mL 0.1730 mL 0.3460 mL 0.8651 mL
    100 mM 0.0277 mL 0.1384 mL 0.2768 mL 0.6921 mL
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    • 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.

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    Product Name:
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    Cat. No.:
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