| Name | Varespladib |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 60 mg/mL (157.73 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Varespladib | sPLA2 | secretory | Recombinant | PLA2 | Phospholipase | nonpancreatic | LY-315920 | LY 315920 | Inhibitor | inhibit | IIA | human | hnsPLA2 | group | anti-inflammatory |
| Inhibitors Related | Neomycin sulfate | Levamisole hydrochloride | 1-Naphthaleneacetic acid potassium salt | Difluprednate | trans-Benzylideneacetone | Benzylideneacetone | Omeprazole | Indomethacin | Darapladib | 1-Naphthaleneacetic acid | Lansoprazole | Magnesium sulfate |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Pediatric Drug Library | ReFRAME Related Library | Anti-Obesity Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library |
United States
