别名: 伐瑞拉迪对照品
英文名:Varespladib(LY315920,LY-333013)
Chemical Name: [[3-(Aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]acetic acid
分子式:C21H20N2O5
分子量: 380.40
Appearance:White powder
Solubility:Soluble in DMSO
纯度: >99%
储存条件: at -20℃ 2 years
CAS No: 172732-68-2
Biological Activity:
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.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.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 nM. Therefore£¬the use of Varespladib have a beneficial effect in preventing various inflammatory disease states.