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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $38 | In Stock | |
5 mg | $89 | In Stock | |
10 mg | $147 | In Stock | |
25 mg | $239 | In Stock | |
50 mg | $355 | In Stock | |
100 mg | $513 | In Stock | |
1 mL x 10 mM (in DMSO) | $106 | In Stock |
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. |
Alias | LY315920 |
Molecular Weight | 380.39 |
Formula | C21H20N2O5 |
Cas No. | 172732-68-2 |
Smiles | CCc1c(C(=O)C(N)=O)c2c(OCC(O)=O)cccc2n1Cc1ccccc1 |
Relative Density. | 1.32 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 60 mg/mL (157.73 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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