SML1100

Varespladib

≥98% (HPLC), Secretory phospholipase A2 inhibitor, powder

• Synonym(s): 2-[[3-(2-Amino-2-oxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]-acetic acid, A-001, LY-315920, LY315920
• Empirical Formula (Hill Notation): C₂₁H₂₀N₂O₅
• CAS Number: 172732-68-2
• Molecular Weight: 380.39
• UNSPSC Code: 41106300
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Product Name: Varespladib, ≥98% (HPLC)
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 10 mg/mL, clear
• storage temp.: −20°C
• SMILES string: [Na+].[n]2(c3c(c(ccc3)OCC(=O)[O-])c(c2CC)C(=O)C(=O)N)Cc1ccccc1
• InChI: 1S/C21H20N2O5.Na/c1-2-14-19(20(26)21(22)27)18-15(9-6-10-16(18)28-12-17(24)25)23(14)11-13-7-4-3-5-8-13;/h3-10H,2,11-12H2,1H3,(H2,22,27)(H,24,25);/q;+1/p-1
• InChI key: XZZUHXILQXLTGV-UHFFFAOYSA-M

Description

Application

Varespladib has been used as a secretory phospholipase A (sPLA2) inhibitor:

• to test its effect on the human astrocytes subjected to psychosine-induced toxicity
• to test its neutralization functionality on the black snake species P. colletti venom
• in combination with snake venom metalloproteinases (SVMP)-inhibitor, marimastat to test its protective functionality on envenoming by vipers

Biochem/physiol Actions

Varespladib is a potent and selective inhibitor of secretory phospholipase A2 (sPLA2).

Varespladib is a potent and selective inhibitor of secretory phospholipase A2 (sPLA2). The compound Varespladib inhibits both human and mouse sPLA2 group IIA, V, and X enzymes at low nM concentrations.

Varespladib is effective against viper and elapid venoms and is used in snakebite therapy. It is reported to interact with the hydrophobic channel of the PLA2-like toxin in in vitro structural studies. It blocks inflammatory cascades related to the sPLA2.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable