spla2-iia

sPLA2-X Inhibitor 31 is a selective inhibitor of secreted phospholipase A2 type X (sPLA2-X) (IC50s of 26 nM, 310 nM, and 2230 nM for sPLA2-X, sPLA2-IIa, and sPLA2-V, respectively).

sPLA2-IIA Inhibitor 是 FLSYK 的环状五肽类似物，具有环2-Nal-Leu-Ser-2-Nal-Arg (c2) 结构，能够特异性结合 hGIIA（人类 IIA 磷脂酶 A2），有效抑制其酯键水解活性。该化合物作为酯酶超家族的一员，主要作用于甘油磷脂 sn-2 位置的酯键，从而阻断游离脂肪酸和花生四烯酸等物质的释放。

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。

Tanshinone I (Tanshinone A) 是IIA 型人重组sPLA2(IC50=11 μM)和兔重组cPLA2(IC50=82 μM)抑制剂。

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。

KH064 is a sPLA2-IIA inhibitor of oral activity.

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.

12-HETE ((±)12-HETE) 是 PGE2 的调节因子，具有抗血栓形成和促血栓形成作用，通过蛇毒 IIA 组磷脂酶 A2 诱导诱导 PGE2 释放和 COX-2 表达。12-HETE 还是一种神经调节剂，通过激活 NADPH 氧化酶和随后的生成激活视网膜细胞，诱导糖尿病视网膜病变的内皮功能障碍。

Phosphatidylethanolamines are important components of cell membranes and biochemical pathways of fatty acid synthesis. 1-Palmitoyl-2-linoleoyl PE (PLPE) is one of the many phosphatidylethanolamines that may be present in cellular membranes. It has been used in studies involving the biosynthesis of anandamide via the phospholipase A2 (PLA2) and lysoPLD pathways. PLPE can also be used as a specific substrate to assess the activity of sPLA2-IIA in the presence of other phospholipids.

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.