soluble epoxide hydrolase

N-(3-methoxybenzyl)-octadecanamide 从玛卡 (Lepidium meyenii Walp.) 转化而来。

Soluble epoxide hydrolase inhibitor is a soluble epoxide hydrolase inhibitor (human soluble epoxide hydrolase (h-sEH) with pIC50 of 8.4).

Soluble epoxide hydrolase (sEH) PROTAC 1a是一种利用蛋白质降解靶向嵌合体(PROTAC)技术，通过连接区域将cereblon配体1与sEH抑制剂t-TUCB结合。该化合物通过促进sEH的降解，特异性抑制sEH的水解酶活性(IC50 = 0.8 nM)，相较于其磷酸酶活性(IC50 = >10,000 nM)具有较高选择性。sEH PROTAC 1a还特定促进细胞质中而非过氧体中的sEH降解，并通过溶酶体而非蛋白酶体实现其降解。它能够降低thapsigargin诱导的HepG2与293T细胞中磷酸化的inositol-requiring enzyme 1α (IRE1α)水平和X-box结合蛋白1 (XBP1)剪接，表明能减少ER应激。

EC5026 (BPN-19186) 是首创的，非阿片类的，可溶性环氧水解酶 (sEH) 抑制剂，它可有效缓解发炎性和神经性疼痛。

Dual FAAH sEH-IN-1 是具有高度亲和力的sEH(可溶性环氧水解酶) (IC50: 9.6 nM) 和FAAH(脂肪酸酰胺水解酶) (IC50: 7 nM) 双重抑制剂，具有抗炎活性。

(Rac)-EC5026 ((Rac)-BPN-19186) 是一种有效的可溶性环氧水解酶 (sEH) 哌啶抑制剂，Ki 值为 0.06 nM。(Rac)-EC5026 可用于帕金森氏病和路易体痴呆 (DLB) 的研究。

N,N'-Dicyclohexylurea (AURORA KA-3582) 是一种可溶性环氧化物水解酶 (sEH) 抑制剂。

BI-1935 是可溶性环氧化物水解酶抑制剂，用于与心血管疾病相关的疾病的研究。

CAY10640 (sEH inhibitor-1)一种有效的、具有口服活性、可溶于水的环氧化物水解酶 (sEH) 抑制剂，对人和鼠中的sEH 具有抑制作用，IC50s 分别为 0.4 和 5.3 nM。

sEH inhibitor-7是一种可溶性环氧化物水解酶（sEH）抑制剂，对人和小鼠的 sEH 有抑制作用，IC 50 s 分别为 6.2 μM 和0.15 μM 。sEH inhibitor-7与抗炎活性分子有关。

Diflapolin 是高活性的双 5-脂氧合酶激活蛋白(FLAP) 可溶性环氧化物水解酶抑制剂，具有显著的抗炎作用和较高的靶向选择性。它抑制分离的 sEH 的活性，IC50为20 nM。它还抑制完整人单核细胞和中性粒细胞中 5-LOX 产物的形成，IC50分别为 30 和 170 nM。

CUDA 是一种可溶性环氧水解酶抑制剂，对小鼠 sEH 和人 sEH 作用的 IC50分别为 11.1 和 112 nM。它能选择性地上调过氧化物酶体增殖激活受体 PPARα的活性，有用于心血管疾病的研究潜力。

SWE101 is a potent human and rat soluble epoxide hydrolase (sEH)-P inhibitor(IC50s of 4 μM and 2.8 μM, respectively).

AR-9281 (APAU) 是选择性的可溶性环氧化物水解酶抑制剂，可用于研究高血压和 2 型糖尿病。

trans-AUCB (t-AUCB) 是口服具有活力的、选择性的可溶性环氧水解酶 (sEH) 抑制剂，对人，小鼠和大鼠的 sEH 的IC50分别为 1.3 nM，8 nM，8 nM。它具有抗神经胶质瘤特性。

UC-1728 (t-TUCB) 是一种兔子可溶性环氧化物水解酶抑制剂，兔子肝脏中测得其IC50=2 nM。

DJ-53 (compound 68)为一种口服型基于苯基喹啉的溶性环氧水解酶抑制剂。

LQ-38，一种口服有效的可溶性环氧化物水解酶 (sEH) 抑制剂，其IC50值为5.2 nM。在大鼠足部水肿模型及小鼠急性胰腺炎模型中，LQ-38显现出明显的抗炎效果。此外，在Acetic acid诱导的小鼠扭体模型中，该化合物亦展现了良好的镇痛活性。

sEH inhibitor-19 (Compound (R)-14i) 是一种口服有效的可溶性环氧化物水解酶 (sEH) 抑制剂，IC50值为1.2 nM。sEH inhibitor-19 能抑制 TNF-α 和 IL-6 的表达，并在小鼠急性胰腺炎或Carrageenan诱导的水肿模型中展现出抗炎活性。

sEH-IN-12 is an effective inhibitor of the enzyme soluble epoxide hydrolase (sEH).

(±)12(13)-DiHOME is the diol form of (±)12(13)-EpOME , a cytochrome P450-derived epoxide of linoleic acid also known as isoleukotoxin. [1] It is formed from 12(13)-EpOME by soluble epoxide hydrolase (sEH) in neutrophils. [2] 12(13)-DiHOME is toxic to Sf21 cells expressing sEH and to lacZ-expressing control cells, unlike isoleukotoxin, which is only toxic to cells containing sEH.[1] [2] Levels of 12(13)-DiHOME are increased in rat spinal cord following burn injury, and it enhances cold tolerance, increases fatty acid uptake into brown adipocytes, and decreases serum triglyceride levels in mice. Levels are also elevated in bronchoalveolar lavage fluid (BALF) in humans following exposure to biodiesel exhaust and in exhaled breath condensate in patients with allergic asthma following allergen exposure.[5] [6] Plasma levels of 12(13)-DiHOME are increased immediately following moderate-intensity exercise in mice and humans, an effect that can be prevented by brown adipose tissue removal in the mouse.[7]

Cytochrome P450 metabolism of polyunsaturated fatty acids produces numerous bioactive epoxide regioisomers. (±)10(11)-EpDPA is a docosahexaenoic acid epoxygenase metabolite, derived via epoxidation of the 10,11-double bond of DHA. It has been detected in rat brain and spinal cord, as well as human serum, and acts as a substrate for soluble epoxide hydrolase with a Km value of 5.1 μM. (±)10(11)-EpDPA and other epoxy metabolites of DHA are reported to demonstrate antihyperalgesic activity in inflammatory and neuropathic pain models and to potently inhibit angiogenesis and tumor growth in in vitro assays.

Cytochrome P450 metabolism of polyunsaturated fatty acids produces numerous bioactive epoxide regioisomers. (±)13(14)-EpDPA is a docosahexaenoic acid epoxygenase metabolite, derived via epoxidation of the 13,14-double bond of DHA. It has been detected in rat brain and spinal cord and is a preferred substrate for soluble epoxide hydrolase with a Km value of 3.2 μM. (±)13(14)-EpDPA demonstrates antihyperalgesic activity in inflammatory and neuropathic pain models. (±)13(14)-EpDPA and other epoxy metabolites of DHA are also reported to potently inhibit angiogenesis and tumor growth in in vitro assays.

Docosahexaenoic acid is the most abundant ω-3 fatty acid in neural tissues, especially in the brain and retina. (±)7(8)-EpDPA is an epoxide derivative of DHA that is generated by the action of cytochrome P450 epoxygenases. It is naturally occurring in plasma and brain and spinal cord tissues and is increased following dietary supplementation with ω-3 fatty acids. (±)7(8)-EpDPA and other epoxy metabolites of DHA modulate receptor and channel activities to evoke diverse effects, such as promoting vasodilation, inhibiting angiogenesis, and decreasing inflammatory and neuropathic pain. (±)7(8)-EpDPA is a substrate of soluble epoxide hydrolase (KM = 15 μM), which converts it to the corresponding diol.