phospholipase a2, group iia

Varespladib (LY315920) 是选择性group IIA, secretory phospholipase A2(sPLA2)抑制剂，其IC50=9 nM。它对大鼠，兔，豚鼠和人等各种物种血清的sPLA2活性具有明显的抑制作用，IC50分别为 8.1 nM，5.0 nM，3.2 nM 和 6.2 nM。

GK241 (compound 31a-c) 为一种2-氧代酰胺衍生的化学物质，展现了对人类与小鼠的IIA组分泌型磷脂酶A2（GIIA sPLA2）具有显著的抑制作用（IC50为143 nM与68 nM），其抑制机制已通过分子动力学模拟得到探讨。

CGP 43182 is an effective inhibitor of group IIA secretory phospholipase A2 (Group IIA sPLA2) activity in vitro, which can be used to prevent the synergistic effect of pro-inflammatory genes stimulated by cytokines mediated by NFkappaB.

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs). Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively). Its action is reversible and selective, as pyrrophenone inhibits the secretory type IB and IIA PLA2s with more than a hundred-fold less potency. Pyrrophenone has also been shown to inhibit calcium ionophore (A23187)-stimulated AA release from monocytic cells, interleukin-1-induced PGE2 synthesis in mesangial cells, and the production of PGE2, LTs, and platelet-activating factor by human neutrophils, always with maximal inhibition at concentrations below 1 μM.

Varespladib sodium (LY315920 sodium) is a highly potent and selective inhibitor of group IIA secretory phospholipase A2 (sPLA2), with an IC50 of 9 nM. It demonstrates significant inhibitory activity against sPLA2 in serum samples from multiple species, including rat, rabbit, guinea pig, and human, with IC50 values of 8.1 nM, 5.0 nM, 3.2 nM, and 6.2 nM, respectively.