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Varespladib (LY315920)HnsPLA inhibitor,potent and selective

Varespladib (LY315920)

Catalog No. A4356
Size Price Stock Qty
5mg $65.00 In stock
10mg $120.00 In stock
25mg $290.00 In stock
50mg $520.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Varespladib (LY315920)

Biological Activity

Description Varespladib is a potent and selective inhibitor of human non-pancreatic secretory phospholipase A2 (hnsPLA) with IC50 value of 7 nM.
Targets hnsPLA          
IC50 7 nM          

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Chemical Properties

Cas No. 172732-68-2 SDF Download SDF
Chemical Name 2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetic acid
Canonical SMILES CCC1=C(C2=C(N1CC3=CC=CC=C3)C=CC=C2OCC(=O)O)C(=O)C(=O)N
Formula C21H20N2O5 M.Wt 380.39
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

IC50: 9 ± 1 nM or 7.3 x 10-6 mole fraction for sPLA2 activity

Phospholipases (PLAs) produce rate-limiting precursors in the various types of biologically active lipid biosynthesis. Increased levels of human nonpancreatic secretory phospholipase A2 (hnps-PLA2) have been detected in several pathological conditions. LY315920 was selected for evaluation clinically as an hnps-PLA2 inhibitor.

In vitro: The true potency of LY315920 was defined to be a mole fraction of 1.5 x 10-6 using a deoxycholate/phosphatidylcholine assay. LY315920 was found to be 40-fold less active against human, group IB, pancreatic sPLA2 and was inactive against cytosolic PLA2 and the constitutive and inducible forms of cyclooxygenase. Human sPLA2-induced thromboxane A2 release from isolated guinea pig lung bronchoalveolar lavage cells was inhibited by LY315920 with the IC50 of 0.79 μM [1].

In vivo: The i.v. administration of LY315920, 5 min before the bronchoalveolar lavage cells harvest, led to the inhibition of sPLA2-induced production of TXA2 with an ED50 of 16.1 mg/kg. [2].

Clinical trials: Varespladib methyl, an oral prodrug of LY-315920, effectively reduced LDL-C and inflammatory biomarkers in ACS patients treated with conventional atorvastatin therapy. There were no treatment differences in clinical cardiovascular events [2].

References:
[1] Snyder DW, Bach NJ, Dillard RD, Draheim SE, Carlson DG, Fox N, Roehm NW, Armstrong CT, Chang CH, Hartley LW, Johnson LM, Roman CR, Smith AC, Song M, Fleisch JH.  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;288(3):1117-24.
[2] Rosenson RS, Hislop C, Elliott M, Stasiv Y, Goulder M, Waters D.   Effects of varespladib methyl on biomarkers and major cardiovascular events in acute coronary syndrome patients. J Am Coll Cardiol. 2010;56(14):1079-88.