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Varespladib

Catalog No. T2044 CAS 172732-68-2

Synonyms: LY315920

Varespladib (LY315920), a specific and effective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor(IC50=7 nM), has been investigated for the treatment and prevention of sickle cell disease, vaso-occlusive crisis, and acute coronary syndrome.

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Varespladib, CAS 172732-68-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 313.00
50 mg	In stock	$ 493.00
100 mg	In stock	$ 723.00
1 mL * 10 mM (in DMSO)	In stock	$ 128.00

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Purity: 100%

Biological Description

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Description	Varespladib (LY315920), a specific and effective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor(IC50=7 nM), has been investigated for the treatment and prevention of sickle cell disease, vaso-occlusive crisis, and acute coronary syndrome.
Targets&IC50	hnsPLA2:7 nM
In vitro	In transgenic mice expressing human sPLA2, oral or intravenous administration of LY315920 (0.3-3 mg/kg) effectively inhibits serum sPLA2 activity in a dose-dependent manner.
In vivo	In the absence of human sPLA2 in BAL cells, LY315920 (0.1 μM-3 μM) effectively suppresses thrombus formation regulated by human sPLA2 in a concentration-dependent manner. Additionally, in a human conjunctival epithelial cell line, LY315920 (10 μM) significantly inhibits the expression of membrane-bound mucin MUC16 induced by all-trans-retinoic acid (RA). LY315920 also markedly inhibits sPLA2 activity across various animal serums, demonstrated by its IC50 values: 8.1 nM in rats, 5.0 nM in rabbits, 3.2 nM in guinea pigs, and 6.2 nM in humans.

Synonyms	LY315920
Molecular Weight	380.39
Formula	C21H20N2O5
CAS No.	172732-68-2

Storage

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

Solubility Information

DMSO: 71 mg/mL (186.7 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Draheim SE, et al. J Med Chem. 1996, 39(26), 5159-5175. 2. Snyder DW, et al. J Pharmacol Exp Ther. 1999, 288(3), 1117-1124. 3. Hori Y, et al. Invest Ophthalmol Vis Sci. 2005, 46(11), 4050-4061.

Citations

1. Tan C H, Lingam T M C, Tan K Y. Varespladib (LY315920) rescued mice from fatal neurotoxicity caused by venoms of five major Asiatic kraits (Bungarus spp.) in an experimental envenoming and rescue model. Acta Tropica. 2021: 106289.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Human Metabolite Library Preclinical Compound Library Lipid Metabolism Compound Library Bioactive Compound Library NO PAINS Compound Library Anti-Obesity Compound Library Pediatric Drug Library Immunology/Inflammation Compound Library

Related Products

Related compounds with same targets

Rhamnetin PACOCF3 ML299 hnps-PLA Inhibitor 5-HT1A modulator 1 ML348 Lp-PLA2-IN-15 VU 0364739 hydrochloride

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Keywords

Varespladib 172732-68-2 Metabolism Phospholipase group LY315920 inhibit PLA2 sPLA2 nonpancreatic anti-inflammatory LY-315920 Recombinant human LY 315920 Inhibitor secretory IIA inhibitor

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