faah in 1

FAAH-IN-1 is a fatty acid amide hydrolase (FAAH) inhibitor, with IC50s of 145 nM and 650 nM for rat and human FAAH, respectively.

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。

CB2R FAAH modulator-1是一种大麻素2型受体(CB2R)激动剂，同时也是脂肪酸酰胺水解酶(FAAH)抑制剂（IC50=4 μM），可减少促炎和增加抗炎细胞因子的产生，常用于炎症研究。对 CB2R 和 CB1R 的Kis 分别为14.8 nM 和241.3 nM。

FAAH inhibitor 1 (Benzothiazole analog 3) 是一种有效的脂肪酸酰胺水解酶抑制剂，IC50 为 18 nM。

FAAH MAGL-IN-1, also known as compound SIH 3, is a highly effective inhibitor of FAAH (fatty acid amide hydrolase) and MAGL (monoacylglycerol lipase). It exhibits IC50 values of 31 nM and 29 nM against FAAH and MAGL, respectively. This compound shows promising potential for advancing research in the field of neuropathic pain [1].

FAAH cPLA2α-IN-1为FAAH及cPLA2α的双重抑制剂，IC50值分别为32 nM和47 nM。

Oleoyl proline is an N-acyl amine that can be detected in bovine brain extracts and D. melanogaster larvae using mass spectrometry. In a preclinical model of pain, mice lacking fatty acid amide hydrolase (FAAH KO) had decreased N-oleoyl proline levels in

URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme. However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 μM. There is evidence that the MAGL inhibitory activity of URB754 may be attributed to the impurity bis(methylthio)mercurane (IC50 = 11.9 nM for rat recombinant MAGL) that is found in commercial preparations. URB754 inhibits rat brain fatty acyl amide hydrolase (FAAH) with an IC50 value of 32 μM and binds weakly to the rat central cannabinoid (CB1) receptor with an IC50 value of 3.8 μM. It does not inhibit COX-1 or COX-2 at concentrations up to 100 μM. Inhibition of MAGL hydrolysis of 2-arachidonoyl glycerol (2-AG) is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.

Arachidonoyl 2-chloroethylamide (ACEA) is a potent and selective cannabinoid (CB) receptor 1 agonist with Ki values of 1.4 and >2,000 nM for CB1 and CB2 receptors, respectively. In whole animal experiments, ACEA induces hypothermia in mice with the same efficacy as arachidonoyl ethanolamide , in spite of its higher affinity for the CB1 receptor. These data have been interpreted to indicate that ACEA may be a substrate for fatty acid amide hydrolase (FAAH), and thus only transiently available in whole animal experiments.

N-(1-(3,4-Dihydroxyphenyl)propan-2-yl)oleamide binds to the cannabinoid 1 (CB1) receptor with a Ki value of 365 nM in a radioligand binding assay using rat brain homogenate. It has an EC50 value of 698 nM for the peroxisome proliferator-activated receptor α (PPARα) in a luciferase reporter assay and, in rats, it decreases food intake. It does not inhibit fatty acid amide hydrolase (FAAH).

N-Benzylpalmitamide (Macamide 1) 是从玛卡中得到的一种生物碱，可以时间依赖性方式抑制脂肪酸酰胺水解酶，有治疗疼痛、炎症和中枢神经系统退行性疾病的研究潜力。

FAAH MAGL-IN-2 是一种有效的，可逆的，具有口服活性且可透过血脑屏障的 FAAH 和 MAGL 抑制剂，其IC50值分别为 11 nM 和 36 nM (b>Ki 值分别为 28 nM 和 60 nM)。FAAH MAGL-IN-2 有研究神经性疼痛的潜力而不引起运动障碍。

Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg ml, respectively) but does not inhibit fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM. It also inhibits fatty acid synthase (FASN; Kiapp = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner. Orlistat (10 mg kg) decreases serum cholesterol levels and total bod......

FAAH-IN-8 (compound 11) is a competitive inhibitor of FAAH with an IC50 of 6.7 nM and a Ki of 5 nM. It exhibits high blood-brain permeability and a significant antioxidant profile without neurotoxicity [1].