172733-42-5

172733-42-5 structure

Name: Varespladib sodium
Chemical Name: sodium,2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetate
CAS Number: 172733-42-5
Molecular Formula: C₂₁H₁₉N₂NaO₅
Molecular Weight: 402.37600
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phospholipase
Create Date: 2017-01-16 23:26:59
Modify Date: 2024-01-09 06:02:57
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[1].

Name	sodium,2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetate
Synonyms	UNII-F6M52CDT0W Varespladib sodium

Description	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[1].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase Research Areas >> Inflammation/Immunology
Target	sPLA2:9 nM (IC50)
In Vitro	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]. Western Blot Analysis[2] Cell Line: HCjE cells Concentration: 10 μM Incubation Time: 24 hours, 48 hours Result: Significantly inhibited the RA-induced MUC16 protein expression at both time points. RT-PCR[2] Cell Line: HCjE cells Concentration: 10 μM Incubation Time: 24 hours, 48 hours Result: Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.
In Vivo	Varespladib sodium treatment inhibits human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells with an IC50 of 0.79 μM. And the ED50 for Varespladib sodium is 16.1 mg/kg[1]. Animal Model: Male Hartley guinea pigs (300-500 g)[1] Dosage: 3 mg/kg, 10 mg/kg, and 30 mg/kg Administration: Intravenous injection (Pharmacokinetic study) 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.
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. [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.

Molecular Formula	C₂₁H₁₉N₂NaO₅
Molecular Weight	402.37600
Exact Mass	402.11900
PSA	114.45000
LogP	1.74900

172733-08-3

172733-42-5

Literature: SHIONOGI and CO., LTD.; ELI LILLY AND COMPANY Patent: EP1058547 B1, 2005 ; Location in patent: Page/Page column 5 ;

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