PGE Synthase

ML388 is an inhibitor of human NAD(+)- dependent 15- hydroxyprostaglandin dehydrogenase.

Zomepirac is a prostaglandin synthetase inhibitor. Zomepirac is an orally effective nonsteroidal anti-inflammatory drug (NSAID) that has antipyretic actions.

AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7 macrophages when used at a concentration of 500 μM.2,3AMK (20 mg/kg) decreases MPTP-induced increases in lipid peroxidation in the cytosol and mitochondria from substantia nigra and striatum in a mouse model of MPTP-induced Parkinson’s disease.4 1.Schaefer, M., and Hardeland, R.The melatonin metabolite N1-acetyl-5-methoxykynuramine is a potent singlet oxygen scavengerJ. Pineal Res.46(1)49-52(2009) 2.Kelly, R.W., Amato, F., and Seamark, R.F.N-acetyl-5-methoxy kynurenamine, a brain metabolite of melatonin, is a potent inhibitor of prostaglandin biosynthesisBiochem. Biophys. Res. Commun.121(1)372-379(1984) 3.Mayo, J.C., Sainz, R.M., Tan, D.-X., et al.Anti-inflammatory actions of melatonin and its metabolites, N1-acetyl-N2-formyl-5-methoxykynuramine (AFMK) and N1-acetyl-5-methoxykynuramine (AMK), in macrophagesJ. Neuroimmunol.165(1-2)139-149(2005) 4.Tapias, V., Escames, G., López, L.C., et al.Melatonin and its brain metabolite N1-acetyl-5-methoxykynuramine prevent mitochondrial nitric oxide synthase induction in parkinsonian miceJ. Neurosci. Res.87(13)3002-3010(2009) 5.Tan, D.-X., Manchester, L.C., Reiter, R.J., et al.Melatonin directly scavenges hydrogen peroxide: A potentially new metabolic pathway of melatonin biotransformationFree Radic. Biol. Med.29(11)1177-1185(2000) 6.Hirata, F., Hayaishi, O., Tokuyama, T., et al.In vitro and in vivo formation of two new metabolites of melatoninJ. Biol. Chem.249(4)1311-1313(1974)

mPGES1-IN-4 (compound 32), 作为一种多取代嘧啶类化合物, 主要通过抑制 mPGES-1 实现其抗炎效果，是一种亚微摩尔级别的 PGE2 生产抑制剂，并在体内急性炎症模型中显示了显著的抑制作用。

4-ACETAMIDOANTIPYRINE是一个片段分子，CAS号为83-15-8，可作为分子拼接、扩展和修饰的重要骨架，为新型候选药物的设计与筛选提供结构基础与研究工具，常用于药物发现、药物合成等相关研究。

4‑Acetamidoantipyrine (Standard) 是 4‑Acetamidoantipyrine 的标准品，适用于定量分析、质量控制及生化实验等相关研究。

Zaloglanstat (ISC-27864) is a selective, orally active mPGES-1 inhibitor with an IC50 of 5 nM against human mPGES-1, demonstrating analgesic effects in osteoarthritis and inflammatory arthritis.

HPGDS inhibitor 1 是口服具有活性的HPGDS 选择性抑制剂，在酶和细胞分析中的IC50值分别为 0.6 nM 和 32 nM，但对 L-PGDS、mPGES、COX-1、COX-2 、5-LOX 无抑制作用。

AT56 是口服有活性的脂钙蛋白型前列腺素 D 合酶 (L-PGDS) 选择性抑制剂，其IC50=95 μM，Ki=75 μM。它能够特异性地抑制L-PGDS 催化的 PGD2介导的嗜睡或疼痛反应。

Esflurbiprofen 是 Flurbiprofen 的活性对映体，是 COX-1 和 COX-2 的抑制剂，对 COX-1和 COX-2的 IC50分别为0.48 和 0.47 μM。

HQL-79 is a selective and orally active human hematopoietic prostaglandin D synthase (H-PGDS) inhibitor. It inhibits the synthesis of PGD2 and acts as an anti-allergic agent (Kd: 0.8 μM and IC50: 6 μM). It also shows no obvious effect on COX-1, COX-2, m-P

Heneicosapentaenoic Acid (HPA) is a fatty acid found in small amounts in Bryopsis pennata Lamouroux green algae and fish oils, with a structure similar to eicosapentaenoic acid (EPA), but with an additional carbon at the carboxyl end, resulting in the first double bond being in the Δ6 position. HPA is important for researching the impact of double bond positions in n-3 fatty acids, as it integrates into phospholipids and triacylglycerol in vivo as effectively as EPA and docosahexaenoic acid (DHA), while strongly inhibiting the synthesis of arachidonic acid from linoleic acid. Despite being a poor substrate for prostaglandin H (PGH) synthase and 5-lipoxygenase, HPA can rapidly deactivate PGH synthase. HPA methyl ester, in certain formulations, acts as a prodrug to enhance cellular uptake of HPA before being converted into free acid by esterases, and serves as a useful reference standard.

U-51605, a stable analog of the endoperoxide prostaglandin H2 (PGH2), functions as an inhibitor with greater selectivity towards prostacyclin (PGI) synthase over thromboxane (TX) synthase. It also acts as a partial agonist at TP receptors. Studies show that at a concentration of 2.8 µM, U-51605 effectively inhibits PGI synthase in human foreskin fibroblasts, while a concentration of 5.6 µM is required to inhibit human platelet TX synthase. Furthermore, U-51605, at up to 1 µM, decreases the release of prostacyclin in SHR aorta triggered by the calcium ionophore A-23187 without impacting TXA2 production, and notably enhances the release of PGE2 and PGF2α.

Cannflavin B，一种从Cannabis sativa L. 分离得到的异戊二烯化黄酮，表现出抗炎活性。

4-AcetaMido-d3-antipyrine 是 4-AcetaMido-antipyrine 的氘代化合物。4-AcetaMido-antipyrine 的 CAS 号为 83-15-8。

Sinensetin (Pedalitin permethyl ether) 是从水果中发现的一种甲基化黄酮，有很强的抗血管和抗炎症的能力。

CAY10678 是一种 mPGES-1抑制剂，抑制 PD-1。CAY10678 可减少胶原沉积和T细胞耗竭，可用于研究黑色素瘤。

PGS-IN-1 (KME-4)是一种前列腺素合成酶抑制剂，IC50=0.28 μM。它也可抑制5-脂肪氧合酶的活性，IC50=1.05 μM。

CAY10589 is an mPGES-1 inhibitor.

Vipoglanstat is a prostaglandin E synthase inhibitor and an anti-inflammatory. Vipoglanstat ameliorates leukocyte infiltration and lung injury resulting from both endotoxin-induced and sepsis-induced lung injury.

Pranoprofen (Pyranoprofen) 可抑制COX1/2酶，阻断花生四烯酸转化为二十烷醇，减少前列腺素的合成。它是一种用于眼科的非甾体抗炎试剂。

Suprofen (Suprol) 是一种非甾体抗炎化合物，对前列腺素合成具有抑制作用。

Cafestol 是咖啡特有的一种二萜，可靶向 AP-1 抑制ERK，有化学预防、抗肿瘤、保肝、抗氧化和抗炎作用。它通过抑制NF-kB 活化途径强烈的抑制 PGE2的产生，还抑制 LGE 激活的 RAW264.7 细胞中的PGE2产生和环氧合酶(COX-2)的 mRNA 表达。

Friluglanstat为一种mPGES-1抑制剂，表现出抗炎作用。

Benzydamine 是一种苄基吲唑，具有镇痛、解热和抗炎作用。 Benzydamine 用于减少手术后和创伤后的疼痛和水肿，并促进愈合。

Linderaspirone A shows significant activity against glucosamine-inducedinsulin resistance.

hPGDS-IN-1是 hPGDS 抑制剂，使用荧光偏振检测或通过 EIA 法测得的 IC50值为12 nM。

α-Gracinoic acid 属于mPGES-1抑制剂，表现出抗炎性能。

mPGES1-IN-5 (compound 18) 为亚微摩尔级多取代嘧啶类化合物，其主要通过阻断mPGES-1来发挥抗炎效果，并在体内急性炎症模型中显示出显著的抑制作用，有效抑制PGE2的生成。

LC-R 505 is an anti-inflammatory.

Fagaramide possesses Antiplasmodial activity.

F092 是一种高效的造血前列腺素 D 合成酶 (H-PGDS) 抑制剂， 可以用于研究过敏性炎症和与血管相关的疾病。

PF-9184 是一种有效且高度选择性的人微粒体前列腺素 E 合酶 1 (mPGES-1) 的抑制剂，IC50 值为 16.5 nM。PF-9184 体外抑制 IL-1β 诱导的 PGE2 合成。

mPGES-1 Inhibitor-1 是一种新型的微粒体前列腺素 E 合酶-1（mPGES-1）选择性抑制剂，具有抗炎镇痛活性，可用于研究急性肝损伤。

mPGES1-IN-9 (compound 1_8) 是mPGES1的抑制剂，其IC50为0.5 μM，用于抗炎研究。

FR20 is a human microsomal prostaglandin synthase 1 (mPGES 1) inhibitor.