faah inhibitor 1

FAAH inhibitor 1 (Benzothiazole analog 3) is a potent FAAH inhibitor with an IC50 of 18 nM.

MM-433593 is a selective fatty acid amide hydrolase (FAAH-1) inhibitor for the treatment of pain, inflammation, and other disorders.

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.

JNJ-1661010 (Takeda-25) is an effective and specific FAAH inhibitor (IC50: 10/ 12 nM for rat/human), shows >100-fold selectivity for FAAH-1 than FAAH-2.

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.

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.

OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor with a Ki of 2.4 μM.

Irafamdastat (BMS-986368) [Example 74] is an inhibitor of FAAH and MAGL, with IC50 values of ≤ 100 nM for human FAAH and 100 nM-1 μM for human MAGL. It exhibits anticonvulsant properties.

5-HT6R/FAAH modulator 1 is a selective ligand for the serotonin 5-HT6 receptor and an inhibitor of the fatty acid amide hydrolase (FAAH). It exhibits a pKi of 6.33 for 5-HT6 and a pIC50 of 6.33 for FAAH. This compound also shows mild inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with a pIC50 of 5.12. Additionally, it can inhibit apoptosis and reduce reactive oxygen species (ROS) levels. 5-HT6R/FAAH modulator 1 is applicable in the study of neurological disorders such as Alzheimer's disease (AD).

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.

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.

1-Monomyristin (2,3-Dihydroxypropyl tetradecanoate) , a 1-monoglyceride of myristic acid, has antibacterial activity against several Gram-positive bacterial strains. 1-Myristoyl-rac-glycerol is used in colloidal chemistry as a nonionic surfactant in the development of micelles.

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].

Carpro-AM1 is a compound that acts as a dual inhibitor of both fatty acid amide hydrolase (FAAH) and substrate-selective cyclooxygenase (COX). It exhibits potent inhibitory activity against FAAH, with an IC50 value of 94 nM [1].

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 (T0686) 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 (T0686) 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 (T0686) (10 mg/kg) decreases serum cholesterol levels and total bod......

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].

FAAH Inhibitor 2 (Compound 17b) is an irreversible inhibitor of fatty acid amide hydrolase (FAAH), demonstrating an IC50 value of 0.153 μM [1].

3-Decyl-5,5'-diphenyl-2-thioxo-4-imidazolidinone (compound 45), having a pI50 of 5.89, shows promise as an inhibitor of fatty acid amide hydrolase (FAAH). Despite its activity, it demonstrates a lack of affinity for cannabinoid receptors CB(1) and CB(2) [1].

CAY10435, a β-ketooxazapyridine and selective FAAH inhibitor, exhibits antimicrobial properties. It binds non-competitively to the FAAH of Dictyostelium discoideum, demonstrating a Kd value of 0.57 nM [1] [2].

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].

JNJ-42165279 (dihydrochloride) is an FAAH inhibitor with IC50 values of 70 nM for hFAAH and 313 nM for rFAAH, respectively [1].

AA38-3 (1-Piperidinecarboxylic acid, 4-nitrophenyl ester) inhibites three SHs (ABHD6, ABHD11, and FAAH)