faah in 1

FAAH-IN-1 is a fatty acid amide hydrolase (FAAH) inhibitor with IC50 values of 145 nM for rat FAAH and 650 nM for human FAAH.

Dual FAAH sEH-IN-1 is a dual inhibitor of sEH (soluble epoxide hydrolase) (IC50: 9.6 nM) and FAAH (fatty acid amide hydrolase) (IC50: 7 nM) with high affinity and anti-inflammatory activity.

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 is a dual inhibitor of FAAH and cPLA2α, with potent inhibitory activity, exhibiting half-maximal inhibitory concentrations (IC50s) of 32 nM for FAAH and 47 nM for cPLA2α [1].

CB2R FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

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) inhibits fatty acid amide hydrolase (FAAH) in a time-dependent manner and could potentially offer a good alternative for the treatment of pain, inflammation and CNS degenerative disorders.

FAAH MAGL-IN-2, a potent and reversible inhibitor of FAAH and MAGL, demonstrates oral activity and the ability to cross the blood-brain barrier. It exhibits IC50 values of 11 nM for FAAH and 36 nM for MAGL (Ki values of 28 nM and 60 nM, respectively). This compound shows promise for neuropathic pain research, without impairing locomotion [1].

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].