2. Metabolic Enzyme/Protease
  3. Phospholipase
  4. Varespladib

Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively.

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

CAS No. : 172732-68-2

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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 9 publication(s) in Google Scholar

Other Forms of Varespladib:

Varespladib Related Antibodies

Top Publications Citing Use of Products

    Varespladib purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Sep:237:251-269.  [Abstract]

    Indoximod (20 mg/kg, oral gavage, 14 days) or Varespladib (30 mg/kg, oral gavage, 14 days) resulted in significant weight gain in the BLM-induced mouse model.

    Varespladib purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Sep:237:251-269.  [Abstract]

    Indoximod (20 mg/kg, oral gavage, 14 days) or Varespladib (30 mg/kg, oral gavage, 14 days) markedly improved overall survival compared with the BLM-treated group.

    Varespladib purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Sep:237:251-269.  [Abstract]

    Indoximod (20 mg/kg, oral gavage, 14 days) or Varespladib (30 mg/kg, oral gavage, 14 days) reversed visual pulmonary injury and collagen deposition, attenuated the increase in lung coefficient, and prevented the reduction in terminal body weight in the BLM-induced mouse model.

    Varespladib purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Sep:237:251-269.  [Abstract]

    Indoximod (20 mg/kg, oral gavage, 14 days) or Varespladib (30 mg/kg, oral gavage, 14 days) reversed the BLM-induced upregulation of Pla2g2a, Ido1, Acta2, and Col1a1 gene expression.

    Varespladib purchased from MedChemExpress. Usage Cited in: Clin Nutr. 2024 Jul;43(7):1725-1735.  [Abstract]

    Varespladib (intragastric administration, 10 mg/kg, once daily for two weeks) decreased blood glucose and serum insulin levels in aged mice, but not in young adult mice.

    Varespladib purchased from MedChemExpress. Usage Cited in: Clin Nutr. 2024 Jul;43(7):1725-1735.  [Abstract]

    Western blot analysis of p-AKT, total AKT, and GAPDH in the liver, white adipose tissue (WAT), and skeletal muscle of vehicle- or varespladib-administered (intragastric administration, 10 mg/kg, once daily for two weeks) 15-month-old mice with or without insulin stimulation.

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    • References

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    Description

    Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively[1].

    IC50 & Target[1]

    sPLA2

    9 nM (IC50)

    In Vitro

    Varespladib (10 μM; 24 and 48 hours; HCjE cells) treatment results in complete inhibition of the RA-induced increase in MUC16 protein detected in cell lysates at both time points[2].
    Varespladib (10 μM; 24 and 48 hours; HCjE cells) treatment significantly inhibits RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours[2].

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

    Varespladib Related Antibodies

    Western Blot Analysis[2]

    Cell Line: HCjE cells
    Concentration: 10 μM
    Incubation Time: 24 hours and 48 hours
    Result: Significantly inhibited the RA-induced MUC16 protein expression at both time points.

    RT-PCR[2]

    Cell Line: HCjE cells
    Concentration: 10 μM
    Incubation Time: 24 hours and 48 hours
    Result: Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.
    In Vivo

    Varespladib treatment inhibits human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells with an IC50 of 0.79 μM. And the ED50 for Varespladib is 16.1 mg/kg[1].

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

    Animal Model: Male Hartley guinea pigs (300-500 g)[1]
    Dosage: 3 mg/kg, 10 mg/kg, and 30 mg/kg
    Administration: Intravenous injection (Pharmacokinetic study)
    Result: Consistent inhibition of sPLA2 activity in BAL fluid was observed. Reduced the human sPLA2-induced generation of TXA2 on BAL cells from guinea pigs.
    Clinical Trial
    Molecular Weight

    380.39

    Formula

    C21H20N2O5
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(O)COC1=CC=CC2=C1C(C(C(N)=O)=O)=C(CC)N2CC3=CC=CC=C3
    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 (262.89 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 2.6289 mL 13.1444 mL 26.2888 mL
    5 mM 0.5258 mL 2.6289 mL 5.2578 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 (6.57 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 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  17% Solutol HS-15 in Saline

      Solubility: 1.5 mg/mL (3.94 mM); Suspended solution; Need ultrasonic

    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).
    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: 99.74%

    SDS (393 KB)

    COA (259 KB) HNMR (141 KB) RP-HPLC (245 KB) LCMS (106 KB)

    Handling Instructions (2659 KB)
    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 2.6289 mL 13.1444 mL 26.2888 mL 65.7220 mL
    5 mM 0.5258 mL 2.6289 mL 5.2578 mL 13.1444 mL
    10 mM 0.2629 mL 1.3144 mL 2.6289 mL 6.5722 mL
    15 mM 0.1753 mL 0.8763 mL 1.7526 mL 4.3815 mL
    20 mM 0.1314 mL 0.6572 mL 1.3144 mL 3.2861 mL
    25 mM 0.1052 mL 0.5258 mL 1.0516 mL 2.6289 mL
    30 mM 0.0876 mL 0.4381 mL 0.8763 mL 2.1907 mL
    40 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6431 mL
    50 mM 0.0526 mL 0.2629 mL 0.5258 mL 1.3144 mL
    60 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0954 mL
    80 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8215 mL
    100 mM 0.0263 mL 0.1314 mL 0.2629 mL 0.6572 mL
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    Varespladib 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:

    Varespladib172732-68-2LY315920LY 315920LY-315920PhospholipaseRecombinanthumangroupIIAnonpancreaticsecretoryPLA2sPLA2anti-inflammatoryInhibitorinhibitorinhibit

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