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.

CB2R/FAAH modulator-2 (compound 26) is a dual modulator targeting at CB2R and FAAH. CB2R/FAAH modulator-2 acts as a CB2R agonist and FAAH inhibitor, the Ki values are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 has studies research value related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.

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/cPLA2α-IN-1 is a compound that simultaneously inhibits both FAAH and cPLA2α, demonstrating potent activity with half-maximal inhibitory concentrations (IC50s) of 32 nM for FAAH and 47 nM for cPLA2α [1].

CB2R/FAAH modulator-3 (compound 27) is a modulator targeting at CB2R and FAAH. CB2R/FAAH modulator-3 acts as a CB2R agonist and FAAH inhibitor, the Ki values are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 has research value related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.

FAAH/MAGL-IN-3 (Compound 10) is an irreversible dual inhibitor of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) that acts on FAAH (IC50: 179 nM) and MAGL (IC50: 759 nM). FAAH/MAGL-IN-3 showed little PAMPA (parallel artificial membrane permeability assay) permeability.

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.

FAAH-IN-2 (O-Desmorpholinopropyl Gefitinib) is a potent inhibitor of FAAH(fatty acid amide hydrolase).

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

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

FAAH-IN-7, a potent and reversible inhibitor of fatty acid amide hydrolase (FAAH), demonstrates significant neuroprotective effects, particularly by mitigating oxidative stress in 1321N1 astrocytes. With an IC50 value of 8.29 nM, it also shows notable efficacy in an ex vivo neuroinflammation model.

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-IN-5 (Compound 7) is a relatively selective, irreversible inhibitor of fatty acid amide hydrolase (FAAH) (IC50: 10.5 nM). FAAH-IN-5 has low PAMPA (parallel artificial membrane permeability assay) permeability.

URB-597 (FAAH Inhibitor II) is an effective, orally bioavailable FAAH inhibitor (IC50: 4.6 nM), and no effect on other cannabinoid-related targets.

URB532 is an irreversible fatty acid amide hydrolase (FAAH) inhibitor.

OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).

MK-4409 is a novel and selective inhibitor of oxazole fatty acid amide hydrolase FAAH.MK-4409 can be used to study inflammatory and neuropathic pain.

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

Biochanin A (4-Methylgenistein) is an isoflavone derivative isolated from red clover Trifolium pratense with anticarcinogenic properties. Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor.

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.

MAGL-IN-4 (His121 ARG57) is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.

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).

FP-biotin is a potent organophosphorus toxicant, ideal for identifying novel biomarkers of organophosphorus toxicant exposure. It measures FAAH, ABHD6, and MAG-lipase activity, specifically in plasma studies, due to the efficient purification of biotinylated peptides through binding to immobilized avidin beads.

JNJ-42165279 covalently inactivates the FAAH enzyme but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 (10 μM) exhibits high selectivity against a panel of 50 receptors, enzymes, transporters, and

4-Nonylphenylboronic acid is a inhibitor of FAAH.

BIA 10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) that increases levels of the neurotransmitter anandamide in the central nervous system and in peripheral tissues (that is, the rest of the body other than the brain and spinal cord). BIA 10-2474(BIA10-2474) interacts with the human endocannabinoid system. BIA 10-2474(BIA10-2474) was in development for the treatment of a range of different medical conditions from anxiety to Parkinson's disease, also for the treatment of chronic pain of multiple sclerosis, Y, hypertension or the treatment of obesity.

ARN272 is a FAAH-like anandamide transporter (FLAT) inhibitor (IC50: 1.8 μM).

LY2183240 inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM). LY2183240 is a novel and highly effective blocker of anandamide uptake (IC50 = 270 pM).

WWL 154 is an serine hydrolase (SH) and fatty acid amide hydrolase FAAH-4 inhibitor.

N-(3-Methoxybenzyl)Palmitamide is a promising FAAH inhibitor, treatment of pain, inflammation and CNS degenerative disorders.

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

Methyl ganoderate A, an inhibitor of Farnesyl protein transferase (FPT) with an IC50 of 38 µM, exhibits potential anticancer effects. Additionally, it inhibits fatty acid amide hydrolase (FAAH), further underscoring its therapeutic potential.

JNJ-40413269 is a competitive inhibitor of fatty acid amide hydrolase (FAAH), which demonstrates robust central target engagement, and shows efficacious in a rat model of neuropathic pain.

N-Benzyllinolenamide is a natural product. It is an inhibitor of fatty acid amide hydrolase (FAAH, IC50 of 41.8 μM).

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.

PF3845yne is an alkyne analogue of PF-3845 maintaining high potency for FAAH.

MAGL-IN-5 is a non-selective lipase inhibitor.

OL-135 is a CNS penetrant, highly potent and selective reversible inhibitor of FAAH. OL-135 exhibits analgesic pharmacology in various animal models without the motor impairment associated with direct CB1 agonism.

Palmitoylisopropylamide is a selective FAAH inhibitor that inhibits [H]-AEA uptake and cell proliferation at low concentrations.

Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester functioning as a central cannabinoid receptor (CB1) antagonist and exhibits equipotent inhibition of fatty acid amide hydrolase (FAAH), with both activities possessing an IC50 value of 2 nM [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].

KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human/mouse/rat MAGL (IC50: 5.9/15/43 nM). It has not inhibitory for FAAH (IC50 > 50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).

PF 750 (ZINC27647189) is a selective and covalent inhibitor of FAAH. PF 750 shows IC50s varying from 16.2 to 595 nM in different incubation times.

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

PF-04457845 is a greatly and effctive FAAH inhibitor, and for hFAAH(IC50=7.2±0.63 nM) and rFAAH(IC50=7.4±0.62 nM).

URB524 is a FAAH inhibitor.

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

JZP-MA-13 is a selective α/β-hydrolase domain 6 (ABHD6) inhibitor, demonstrating impressive specificity with an IC50 value of 392 nM, and exhibits no inhibitory effects on monoacylglycerol lipase (MAGL), ABHD12, fatty acid amide hydrolase (FAAH), or other serine hydrolases. Additionally, JZP-MA-13 serves as a positron emission tomography (PET) ligand for in vivo imaging of ABHD6.

PDP-EA is an activator of fatty acid amide hydrolase(FAAH) and enhances the amidohydrolase activity of FAAH.

Orlistat (Tetrahydrolipstatin) is an Intestinal Lipase Inhibitor. The mechanism of action of orlistat is as a Lipase Inhibitor.