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Varespladib sodium

Catalog No. T39173 CAS 172733-42-5

Synonyms: LY315920 sodium

Varespladib sodium (LY315920 sodium) is a highly potent and selective inhibitor of group IIA secretory phospholipase A2 (sPLA2), with an IC50 of 9 nM. It demonstrates significant inhibitory activity against sPLA2 in serum samples from multiple species, including rat, rabbit, guinea pig, and human, with IC50 values of 8.1 nM, 5.0 nM, 3.2 nM, and 6.2 nM, respectively.

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Varespladib sodium, CAS 172733-42-5

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Description	Varespladib sodium (LY315920 sodium) is a highly potent and selective inhibitor of group IIA secretory phospholipase A2 (sPLA2), with an IC50 of 9 nM. It demonstrates significant inhibitory activity against sPLA2 in serum samples from multiple species, including rat, rabbit, guinea pig, and human, with IC50 values of 8.1 nM, 5.0 nM, 3.2 nM, and 6.2 nM, respectively.
Targets&IC50	sPLA2:9 nM (IC50)
In vitro	Treatment with Varespladib sodium (10 μM; 24 and 48 hours; HCjE cells) completely inhibits the retinoic acid (RA)-induced increase in MUC16 protein expression in HCjE cell lysates at both 24 and 48 hours, as confirmed by Western Blot Analysis and RT-PCR. This indicates a 100% inhibition at 24 hours and a 99% inhibition at 48 hours, demonstrating Varespladib sodium's efficacy in significantly reducing RA-induced MUC16 expression in this cell line at the specified concentrations and time points[2].
In vivo	Varespladib sodium effectively suppresses the release of thromboxane A2 (TXA2) triggered by human sPLA2 from bronchoalveolar lavage cells in isolated guinea pig lungs, with an inhibitory concentration (IC50) of 0.79 μM. Moreover, it has been determined that the effective dose (ED50) of Varespladib sodium is 16.1 mg/kg in male Hartley guinea pigs weighing 300-500 g. When administered intravenously at dosages of 3 mg/kg, 10 mg/kg, and 30 mg/kg, a consistent inhibition of sPLA2 activity in the bronchoalveolar lavage fluid was recorded, alongside a reduction in the sPLA2-induced TXA2 generation in the bronchoalveolar lavage cells of these guinea pigs.

Synonyms	LY315920 sodium
Molecular Weight	403.39
Formula	C21H20N2NaO5
CAS No.	172733-42-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

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Varespladib sodium 172733-42-5 LY315920 sodium inhibitor inhibit

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