LY315920 Inhibitor CAS No. 172732-68-2

Cat. No.	Name	Size	Price
KI0560	LY315920	5 mg	$230
	LY315920	10 mg	$432
	LY315920	50 mg	$1232
	LY315920	200 mg	$3312

Chemical Characteristic

Product Name	LY315920
Synonyms	Varespladib, A-002, LY-333013
CAS No.	172732-68-2
Molecular Weight	380.398
Formula	C₂₁H₂₀N₂O₅
Chemical Name	[[3-(Aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]acetic acid
Smiles	C(=O)(COc1c2c(c(n(c2ccc1)Cc1ccccc1)CC)C(=O)C(=O)N)O
Chemical Structure

Biological activities

LY315920 is a potent, selective inhibitor of recombinant human, group IIA, nonpancreatic secretory PLA2 (sPLA2). LY315920 inhibits sPLA2 activity with an IC50 of 9 nM. LY315920 inhibits human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells with an IC50 of 0.79 μM. LY315920 is 40-fold less active against human, group IB, pancreatic sPLA2 and is inactive against cytosolic PLA2 and the constitutive and inducible forms of cyclooxygenase. The i.v. administration of LY315920, 5 minutes before harvesting the bronchoalveolar lavage cells, results in the inhibition of sPLA2-induced production of TXA2 with an AED_{50 of 16.1 mg/kg. LY315920 suppresses challenge of guinea pig lung pleural strips with sPLA2 produced contractile responses with an apparent KB of 83 nM.^[1] LY315920 significantly inhibits sPLA2 activity present in BALF of neonates.^[2] A high saturated fat, high cholesterol diet guinea pigs treated with LY315920 reduces atherosclerotic lesions by 24%.^[3] LY315920 (1 mg/kg) inhibits PLA2 activity in transgenic mice overexpressing human sPLA2 group IIA in C57BL/6J background. In a high-fat diet model, LY315920 (30 and 90 mg/kg twice a day for 16 weeks) reduces aortic atherosclerosis by 50%. In an accelerated atherosclerosis model, with angiotensin II-induced aortic lesions and aneurysms, LY315920 (30 mg/kg twice a day) reduces aortic atherosclerosis by approximately 40% and attenuates aneurysm formation.^[4] LY315920 decreases atherosclerotic lesion area by ~75% while increasing fibrous cap size by over 200%.^[5]}

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, 288(3): 1117-1124. [2] De Luca D, et al. Varespladib inhibits secretory phospholipase A2 in bronchoalveolar lavage of different types of neonatal lung injury. J Clin Pharmacol. 2012, 52(5): 729-737. [3] Leite JO, et al. A-002 (Varespladib), a phospholipase A2 inhibitor, reduces atherosclerosis in guinea pigs. BMC Cardiovasc Disord. 2009, 9:7. [4] Fraser H, et al. Varespladib (A-002), a secretory phospholipase A2 inhibitor, reduces atherosclerosis and aneurysm formation in ApoE-/- mice. J Cardiovasc Pharmacol. 2009, 53(1): 60-65. [5] Shaposhnik Z, et al. The synergistic inhibition of atherogenesis in apoE-/- mice between pravastatin and the sPLA2 inhibitor varespladib (A-002). J Lipid Res. 2009, 50(4): 623-629.

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