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LY315920 (Varespladib) is a potent and selective secretory phospholipase A2 (sPLA) inhibitor with IC50 of 7 nM. LY315920 inhibited sPLA2 activity with an IC50 of 9 +/- 1 nM or 7.3 x 10(-6) mole fraction, which approached the stiochiometric limit of this assay in a chromogenic isolated enzyme assay. LY315920 (Varespladib) was 40-fold less active against human, group IB, pancreatic sPLA2 and was inactive against cytosolic PLA2 and the constitutive and inducible forms of cyclooxygenase. The i.v. administration of LY315920, 5 min before harvesting the bronchoalveolar lavage cells, resulted in the inhibition of sPLA2-induced production of TXA2 with an ED50 of 16.1 mg/kg. LY315920 (Varespladib) is currently undergoing clinical evaluation and should help to define the role of sPLA2 in various inflammatory disease states.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Transgenic Mice Expressing Human sPLA2 Protein |
| Formulation | 5% DMSO, 5% ethanol, and 30% polyethylene glycol 300 in water |
| Dosages | 0.3–3 mg/kg |
| Administration | i.v. |
| Molecular Weight | 380.39 |
| Formula | C21H20N2O5 |
| CAS Number | 172732-68-2 |
| Solubility (25°C) | DMSO 75 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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