Varespladib
Based on 9 publication(s) in Google Scholar
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.
- Purity: 99.74%
- CAS No.: 172732-68-2
- Formula: C21H20N2O5
- Molecular Weight:380.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Varespladib
More- Cell Metab. 2022 Apr 5;34(4):615-633.e8. [Abstract]
- J Hazard Mater. 2025 Oct 1:499:140027. [Abstract]
- Free Radic Biol Med. 2025 Sep:237:251-269. [Abstract]
- Clin Nutr. 2024 Jul;43(7):1725-1735. [Abstract]
- J Ethnopharmacol. 2024 Jun 12:327:118006. [Abstract]
- J Lipid Res. 2026 Mar 3;67(4):101014. [Abstract]
- J Lipid Res. 2025 Jan 6:100742. [Abstract]
- Toxicon. 2022 Aug:215:69-76. [Abstract]
- Korean J Physiol Pharmacol. 2021 Mar 1;25(2):159-166. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Histological Imaging/Staining
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RT-PCR
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Bio/Physico-chemical Assay
All Phospholipase Isoforms
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Biological Activity
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sPLA2 9 nM (IC50) |
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.
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Cell Line:HCjE cells
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Concentration:10 μM
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Incubation Time:24 hours and 48 hours
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Result:Significantly inhibited the RA-induced MUC16 protein expression at both time points.
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Cell Line:HCjE cells
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Concentration:10 μM
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Incubation Time:24 hours and 48 hours
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Result:Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Hartley guinea pigs (300-500 g)[1]
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Dosage:3 mg/kg, 10 mg/kg, and 30 mg/kg
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Administration:Intravenous injection (Pharmacokinetic study)
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 172732-68-2
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Appearance Solid
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Molecular Weight 380.39
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Formula C21H20N2O5
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Color White to yellow
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SMILES
O=C(O)COC1=CC=CC2=C1C(C(C(N)=O)=O)=C(CC)N2CC3=CC=CC=C3
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Synonyms
LY315920
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Cell Metab
Secreted phospholipase A2 modifies extracellular vesicles and accelerates B cell lymphoma. [Abstract]2022 Apr 5;34(4):615-633.e8. PMID: 35294862 -
J Hazard Mater
Activation of lands cycle-mediated inflammation in living macrophages exposed to label-free particulate matter. [Abstract]2025 Oct 1:499:140027. PMID: 41046674 -
Free Radic Biol Med
Phospholipase A2 group IIA activates Indoleamine 2,3-dioxygenase 1 to drive the progression of pulmonary fibrosis. [Abstract]2025 Sep:237:251-269. PMID: 40473047
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.
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Clin Nutr
Inhibiting arachidonic acid generation mitigates aging-induced hyperinsulinemia and insulin resistance in mice. [Abstract]2024 Jul;43(7):1725-1735. PMID: 38843581
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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J Ethnopharmacol
Hawthorn leaf flavonoids alleviate the deterioration of atherosclerosis by inhibiting SCAP-SREBP2-LDLR pathway through sPLA2-ⅡA signaling in macrophages in mice. [Abstract]2024 Jun 12:327:118006. PMID: 38442806 -
J Lipid Res
EBV promotes alveolar trabecula resorption via extracellular vesicle remodeling by group IIA secreted phospholipase A2. [Abstract]2026 Mar 3;67(4):101014. PMID: 41786250 -
J Lipid Res
Contribution of individual phospholipase A2 enzymes to the cleavage of oxidized phospholipids in human blood plasma. [Abstract]2025 Jan 6:100742. PMID: 39778770 -
Toxicon
Phospholipase A2 inhibitor varespladib prevents wasp sting-induced nephrotoxicity in rats. [Abstract]2022 Aug:215:69-76. PMID: 35724947 -
Korean J Physiol Pharmacol
NOX4/Src regulates ANP secretion through activating ERK1/2 and Akt/GATA4 signaling in beating rat hypoxic atria. [Abstract]2021 Mar 1;25(2):159-166. PMID: 33602886
Solvent & Solubility
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)
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 (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.
Add each solvent one by one: 17% Solutol HS-15 in Saline
Solubility: 1.5 mg/mL (3.94 mM); Suspended solution; Need ultrasonic
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.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Snyder DW, et al. Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI. J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24. [Content Brief]
[2]. Hori Y, et al. Effect of retinoic acid on gene expression in human conjunctival epithelium: secretory phospholipase A2 mediates retinoic acid induction of MUC16. Invest Ophthalmol Vis Sci. 2005 Nov;46(11):4050-61. [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 |
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| 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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