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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 |
| Related Phospholipase Products |
|---|
| ML-298
ML298 is a potent and selective inhibitor of Phospholipase D2 (PLD2) with an IC50 of 355 nM. |
| LCL521
LCL521 is an acid ceramidase (ACDase) inhibitor. |
| SPK-601
SPK-601 (LMV-601) is an inhibitor of the phosphatidylcholine-specific phospholipase C (PC-PLC). |
| CCT129957
CCT129957 is an indole derivative and a potent phospholipase C-γ (PLC-γ) inhibitor with an IC50 of ~3 μM and a GC50 of 15 μM. |
| ONO-RS-082
ONO-RS-082 is an inhibitor of phospholipase A (PLA). |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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