faah (human)

Biochanin A (4-Methylgenistein) 是一种从红三叶车轴草中分离出来的异黄酮衍生物，具有抗癌特性。它是脂肪酸酰胺水解酶抑制剂，作用于小鼠、大鼠和人 FAAH，IC50分别为 1.8、1.4 和 2.4 μM。

JNJ-1661010 (Takeda-25) 是一种有效的、选择性的、可以穿透血脑屏障的脂肪酸酰胺水解酶 (FAAH) 抑制剂，对大鼠和人 FAAH 的 IC50分别为 34 和 33 nM，可用于缓解疼痛的研究。

JZP-361 是一种特异性 MAGL 抑制剂，对人重组 MAGL、人重组 FAAH 和人 hABHD6 的 IC50 分别为 46 nM、7.24 μM 和 1.79 μM。 JZP-361 具有抗组胺活性。 JZP-361可用于哮喘研究。

BIA 10-2474 是一种长效可逆的脂肪酸酰胺水解酶抑制剂，与人类内源性大麻素系统相互作用，可增加中枢神经系统和外周组织，对大鼠大脑不同区域的 IC50值为50至70mg kg。它用于治疗焦虑症、帕金森氏病和多发性硬化症、高血压或肥胖症的慢性疼痛。

KML29 是一种口服具有活性的、高度选择性的不可逆 MAGL 抑制剂，其对小鼠、大鼠和人的 IC50值分别为15 nM、43 nM 和 5.9 nM。它对 FAAH 在内的其他中心和外周丝氨酸水解酶的交叉反应极小。

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.

OMDM-5 是有效的、选择性的anandamide 细胞摄取抑制剂，Ki 为 4.8 μM。它是VR1 (TRPV1)激动剂，EC50为 75 nM，显示出对大麻素 1 型受体 (CB1) 的弱配体活性 (Ki=4.9 μM)。

SA57 is a potent, selective inhibitor of FAAH(IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH).

MK-3168 (12C) 作为一种FAAH抑制剂，对于人类、恒河猴和大鼠展现出了不同的IC50值，分别为1.0、5.5、1.7 nM。该化合物具有优异的脑部摄取能力及对FAAH的高特异性。另外，11C MK-3168 也适用于FAAH PET显像的示踪剂。

AZ513 是一种可逆的FAAH抑制剂，对人类FAAH和大鼠FAAH的IC50分别为551 nM和27 nM。AZ513 在转染人类FAAH的HEK293细胞中抑制花生四烯乙醇胺水解，IC50为360 nM。

JNJ-42165279 是一种 FAAH 抑制剂，抑制 hFAAH 和 rFAAH，IC50分别为70 ± 8 nM 和 313 ± 28 nM。它对其他酶、离子通道、转运蛋白和受体具有高度选择性。

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.

PF-04457845 是一种非常有效的选择性 FAAH 抑制剂，作用于 rFAAH 和 hFAAH，IC50分别为 7.4±0.62 nM 和 7.2±0.63 nM。

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......

Fatty acid amide hydrolase (FAAH), an enzyme responsible for the hydrolysis and inactivation of fatty acid amides like anandamide and oleamide, has been identified as a target by the potent FAAH inhibitor PHOP. PHOP demonstrates remarkable inhibitory activity with K_i values as low as 0.094 nM for human FAAH and 0.2 nM for rat FAAH. Additionally, through a proteomics assay focusing on the serine hydrolase enzyme family, to which FAAH belongs, PHOP's selectivity was evaluated, presenting IC_50 values of 1.1 nM against FAAH, 1.4 nM against triacylglycerol hydrolase (TGH), and greater than 100 µM against an uncharacterized hydrolase (KIAA1363). This specificity profile of PHOP underscores its potential for yielding precise outcomes in studies involving complex biological systems.

AKU-005 是一种针对FAAH和MAGL的双重抑制剂，其对大鼠FAAH和人类FAAH的抑制常数(IC50)分别为63 nM和389 nM。该化合物在探索三叉神经痛觉过敏方面显示出研究潜力。