Research Area
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LY315920(Varespladib) Chemical Structure
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Biological Activity
LY315920(Varespladib) is a selective inhibitor of human, group IIA, nonpancreatic secretory PLA2 (sPLA2). In a chromogenic isolated enzyme assay, Varespladib inhibited sPLA2 activity with an IC50 of 9.6 ±1 nM or 7.3 ×10-6 mole fraction, which approached the stiochiometric limit of this assay. [1]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. [1] Human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells was inhibited by Varespladib with an IC50 of 0.79 mM. [1]Therefore，the use of Varespladib have a beneficial effect in preventing various inflammatory disease states. [1]
References on LY315920(Varespladib)
- [1] J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24
Chemical Information
| Molecular Weight (WM): | 380.39 |
|---|---|
| Formula: | C21H20N2O5 |
| CAS No.: | 172732-68-2 |
| Synonyms: |
LY-315920, LY-333013
|
| Dissolve in (25°C): | DMSO ≥76mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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