phospholipase a2 (pla2)

Varespladib methyl (LY333013) 是 Varespladib 的生物可利用前药，是一种特异性 II 组分泌型磷脂酶 A2 抑制剂。

Lp-PLA2-IN-3 是一种强效且具有口服生物活性的脂蛋白相关磷脂酶 A2（Lp-PLA2）抑制剂，对重组人 Lp-PLA2 具有抑制作用，IC50 值为 14 nM。

Benzylideneacetone 是由昆虫致病细菌 Xenorhabdus nematophila 产生的单萜类化合物，是磷脂酶A2（PLA2）抑制剂，对类花生酸生物合成具有抑制作用，可增强小菜蛾木霉菌的杆状病毒致病性。

N-(p-amylcinnamoyl) Anthranilic Acid (ACA) 是一种广谱磷脂酶 A2(PLA2) 抑制剂，也是TRP channel 的阻滞剂。ACA 也可逆的抑制钙离子激活氯通道 (calcium-activated chloride channels) ，在心律失常方面具有研究的潜力。

1-Linoleoyl Glycerol (Monolinolein) 是脂肪酸甘油。

Lp-PLA2-IN-2 is a selective and potent lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2.

Fludrocortisone acetate (9α-Fludrocortisone acetate) 是一种合成的盐皮质激素，可减少尿液中钠丢失量，也用于增加血压，有用于阿狄森氏病的研究潜力。

Rilapladib (SB 659032) 是 Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) 的选择性抑制剂 (IC50 = 230 pM) 和血小板活化因子受体的拮抗剂。

Anti-Inflammatory Peptide 1 Acetate 在体内具有有效的抗炎活性，是磷脂酶 A2 (PLA2) 的强抑制剂，其存在和活性增加会导致某些身体部位的炎症和疼痛。

ONO-RS-082 是磷脂酶 A 抑制剂。它抑制PLA2的IC50值为1.0 μM，但即使浓度达到 100 μM 也不抑制 PLC。

Luffariellolide 是一种从海洋海绵 Hyrtios communis中获取的萜烯化合物，是人滑膜蛋白磷脂酶A2 (HSF-PLA2) 抑制剂，也是视黄酸受体（RAR） 激动剂。Luffariellolide 抑制缺氧 （1% O2） 诱导的 HIF-1 激活，抑制细胞生长。

PACOCF3 (Palmityltrifluoromet​hylketone) (Palmityltrifluoromethylketone) 是一种钙非依赖性的磷脂酶 A2 (phospholipase A2) 抑制剂，IC50为 3.8 μM。PACOCF3 改变肾小管细胞中的 Ca2+信号传导。

OBAA 是一种有效的磷脂酶 A2 (PLA2) 抑制剂(IC50= 70 nM)，并且在布氏锥虫中阻断 Melittin 诱导的 Ca2+流入(IC50= 0.4 μM)。

Darapladib-impurity 是 Darapladib 的杂质。Darapladib 对脂蛋白相关磷脂酶 A2 (Lp-PLA2)有抑制作用。

9-Oxononanoic Acid是一种氧化脂肪酸，由亚油酸自氧化形成，它能提高磷脂酶 A2（PLA2）的活性，并增加离体人体血浆中血栓素 B2 的生成。9-Oxononanoic Acid 能减少肝脏新脂肪酸的合成，并提高大鼠肝脏肉碱棕榈酰转移酶（β-氧化的标志物）的活性。

Tetranactin is a macrotetrolide and a monovalent cation ionophore that has been found in S. aureus and has antibacterial, insecticidal, and mitogenic activities. It exhibits an equilibrium permeability ratio 1,000-fold greater for lithium than sodium or cesium ions accross bilayer membranes at low voltages. Tetranactin inhibits the growth of Gram-positive bacteria and C. miyabeanus and R. solani fungi when used at concentrations less than 0.9 μg/ml. Tetranactin (0.5-1.5 μg per insect) dose-dependently increases the mortality of adult C. chinensis weevils up to 100% and has mitogenic activity against T. telarius when sprayed onto plants with an LC50 value of 9.2 μg/ml. It reduces IL-1β- and cAMP-induced secretion of phospholipase A2 (PLA2) from rat mesangial cells (IC50s = 43 and 33 nM, respectively). Tetranactin (50 ng/ml) suppresses the proliferation of human T lymphocytes induced by allogeneic cells and IL-2 and supresses the generation of cytotoxic T lymphocytes in mixed lymphocyte cultures. In vivo, tetranactin (10 mg/animal per day) completely inhibits the formation of experimental autoimmune uveoretinitis (EAU) in rats.

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes. AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw. At concentrations as high as 30 μM, AX 048 does not inhibit COX activity or interfere with central cannabinoid receptor signaling.

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.

Phospholipase A2 (PLA2) catalyzes the hydrolysis of phospholipids at the sn-2 position leading to the production of lysophospholipids and free fatty acids. Calcium-dependent cytosolic PLA2 (cPLA2α) is a 85 kDa enzyme that plays a key role in the arachidonic cascade and the inflammatory response associated with this metabolic pathway. CAY10502 is a potent inhibitor of calcium-dependent cytosolic PLA2α (cPLA2α) with an IC50 value of 4.3 nM for the purified enzyme from human platelets. It inhibits arachidonic acid mobilization from A23187-stimulated or TPA-stimulated human platelets with IC50 values of 570 and 0.9 nM, respectively.

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.

Elaidamide is a fatty acid amide that has been found in the cerebrospinal fluid of sleep-deprived cats.1 It inhibits rat microsomal epoxide hydrolase (mEH; Ki = 70 nM).2 Elaidamide also inhibits porcine pancreatic and human synovial phospholipase A2 (PLA2).3 In vivo, elaidamide (10 mg/animal) induces physiological sleep in rats.1References1. Cravatt, B.F., Prospero-Garcia, O., Siuzdak, G., et al. Chemical characterization of a family of brain lipids that induce sleep. Science 268(5216), 1506-1509 (1995).2. Morisseau, C., Newman, J.W., Dowdy, D.L., et al. Inhibition of microsomal epoxide hydrolases by ureas, amides, and amines. Chem. Res. Toxicol. 14(4), 409-415 (2001).3. Jain, M.K., Ghomashchi, F., Yu, B.Z., et al. Fatty acid amides: scooting mode-based discovery of tight-binding competitive inhibitors of secreted phospholipases A2. J. Med. Chem. 35(19), 3584-3586 (1992). Elaidamide is a fatty acid amide that has been found in the cerebrospinal fluid of sleep-deprived cats.1 It inhibits rat microsomal epoxide hydrolase (mEH; Ki = 70 nM).2 Elaidamide also inhibits porcine pancreatic and human synovial phospholipase A2 (PLA2).3 In vivo, elaidamide (10 mg/animal) induces physiological sleep in rats.1 References1. Cravatt, B.F., Prospero-Garcia, O., Siuzdak, G., et al. Chemical characterization of a family of brain lipids that induce sleep. Science 268(5216), 1506-1509 (1995).2. Morisseau, C., Newman, J.W., Dowdy, D.L., et al. Inhibition of microsomal epoxide hydrolases by ureas, amides, and amines. Chem. Res. Toxicol. 14(4), 409-415 (2001).3. Jain, M.K., Ghomashchi, F., Yu, B.Z., et al. Fatty acid amides: scooting mode-based discovery of tight-binding competitive inhibitors of secreted phospholipases A2. J. Med. Chem. 35(19), 3584-3586 (1992).

C22 Glucosylceramide (d18:1 22:0) is an endogenous glucosylceramide. Glucosylceramides are major constituents of skin lipid membranes where they play a role in maintaining the water permeability barrier. They are precursors in the synthesis of lactosylceramide , as well as oligoglycolipids and gangliosides. Phospholipase A2 (PLA2) type XIIA knockdown increases C22 glucosylceramide (d18:1 22:0) expression in rat brain. It is also increased in the brain, but not the liver or spinal cord, of mice fed a methionine-restricted diet. In human athletes, plasma levels of C22 glucosylceramide (d18:1 22:0) increase during exercise and return to basal levels during recovery. This product contains C22 glucosylceramide (d18:1 22:0) isolated from bovine buttermilk.

MJ33 lithium salt 是 NADPH 氧化酶 2 型介导的 ROS 生成抑制剂，是一种氟化磷脂类似物，可抑制过氧化物还蛋白 6 （Prdx6） 的磷脂酶 A2 （PLA2） 活性，可用于研究急性肺损伤。

Protizinic acid 抑制磷脂酶 A2 (PLA2)，IC50值为 210 μM。Protizinic acid 是具有抗炎和解热活性的，口服非甾体抗炎剂。