Varespladib sodium
Based on 9 publication(s) in Google Scholar
Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium 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: 98.83%
- CAS No.: 172733-42-5
- Formula: C21H19N2NaO5
- Molecular Weight:402.38
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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 sodium
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 sodium (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 sodium (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, 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, 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.
Chemical Information
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CAS No. 172733-42-5
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Appearance Solid
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Molecular Weight 402.38
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Formula C21H19N2NaO5
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Color Off-white to light yellow
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SMILES
CCC1=C(C(C(N)=O)=O)C2=C(OCC(O[Na])=O)C=CC=C2N1CC3=CC=CC=C3
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Synonyms
LY315920 sodium
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 sodium 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 sodium 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 sodium 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 sodium 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 sodium 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 sodium 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 : 12.5 mg/mL (31.07 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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: ≥ 1.25 mg/mL (3.11 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.11 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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. 1 [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, 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 | 2.4852 mL | 12.4261 mL | 24.8521 mL | 62.1303 mL |
| 5 mM | 0.4970 mL | 2.4852 mL | 4.9704 mL | 12.4261 mL | |
| 10 mM | 0.2485 mL | 1.2426 mL | 2.4852 mL | 6.2130 mL | |
| 15 mM | 0.1657 mL | 0.8284 mL | 1.6568 mL | 4.1420 mL | |
| 20 mM | 0.1243 mL | 0.6213 mL | 1.2426 mL | 3.1065 mL | |
| 25 mM | 0.0994 mL | 0.4970 mL | 0.9941 mL | 2.4852 mL | |
| 30 mM | 0.0828 mL | 0.4142 mL | 0.8284 mL | 2.0710 mL |
Varespladib sodium Related Classifications
HY-13402A Related Classifications
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