FAAH

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

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

Carprofen (Ridamyl) is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic activities.

<p>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)</p>

LY2183240 inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM).

<p>MAGL-IN-5 is a non-selective lipase inhibitor.</p>

VU534 is a NAPE-PLD agonist with an EC50 of 0.30 μM.VU534 is a dual inhibitor of FAAH and sEH, with an IC50 of 1.2 μM for sEH.VU534 is used in diseases related

2-Chlorophenylboronic acid: A monohalogenated phenylboronic acid used in drug synthesis and as a fatty acid amidase inhibitor.

BuChE-IN-15, a chemical compound, exhibits potent inhibitory activity with IC50 values of 81 nM and 400 nM, respectively. It also demonstrates good blood-brain barrier permeability and neuroprotective properties, making it suitable for research in Alzheimer's disease.

ASP8477 is a potent and selective FAAH inhibitor. It increases anandamide levels in the brain when administered orally. In rat models of neuropathic and osteoarthritic pain, ASP8477 demonstrates significant efficacy without causing motor coordination issues. A single oral dose of ASP8477 improves thermal hyperalgesia and cold allodynia in rats with chronic constriction nerve injury. Moreover, ASP8477 restores the decreased muscle pressure threshold in a myalgia model induced by reserpine. Research indicates that ASP8477 possesses analgesic effects effective for alleviating neuropathic and functional pain, making its pharmacological properties suitable for chronic pain treatment.

FP-biotin: organophosphorus toxicant for biomarker discovery, targets FAAH, ABHD6, MAG-lipase in plasma via avidin-bead purification.

<p>AM6701 is a novel highly potent inhibitor of human alpha/beta hydrolase domain 6 (habhd6)</p>

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

JNJ-42165279 selectively inactivates FAAH without notably affecting other enzymes, ion channels, receptors, or CYPs/hERG at 10 μM.

URB937 is an inhibitor of FAAH and increases anandamide levels(IC50 : 26.8 nM).

1-Monomyristin (2,3-Dihydroxypropyl tetradecanoate) , a 1-monoglyceride of myristic acid, has antibacterial activity against several Gram-positive bacterial

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

<p>JZL195 is a selective and efficacious dual FAAH/MAGL inhibitor.</p>

PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2.

<p>Biochanin A: an isoflavone from red clover with anticancer properties and inhibits FAAH.</p>

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

<p>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).</p>

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.

<p>BIA 10-2474 is a long-acting reversible inhibitor of FAAH that increases levels of the neurotransmitter anandamide in the nervous system.</p>

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

<p>4-Nonylphenylboronic acid is a inhibitor of FAAH.</p>

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

N-Benzylpalmitamide (Macamide 1) inhibits fatty acid amide hydrolase (FAAH) in a time-dependent manner and could potentially offer a good alternative for the

<p>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].</p>

AKU-005 is a dual inhibitor of FAAH and MAGL, exhibiting IC50 values of 63 nM and 389 nM against rat and human FAAH, respectively. This compound has potential for researching trigeminal nociceptive hypersensitivity.

<p>JNJ-40413269 inhibits FAAH, engages central targets, and is effective in rat neuropathic pain.</p>

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

Acetylhydrolase-IN-1 is an inhibitor of the esterase 1-Alkyl-2-acetylglycerophosphocholine (Alkylacetyl-GPC: acetylhydrolase).

<p>OL-135: CNS-accessible, potent, selective FAAH inhibitor with analgesic effects in animals, no motor impairment.</p>

FAAH-IN-7: Reversible FAAH inhibitor, IC50=8.29 nM, reduces oxidative stress, neuroprotective in neuroinflammation.

FAAH-IN-5 (Compound 7) selectively, irreversibly inhibits FAAH (IC50: 10.5 nM) with low PAMPA permeability.

URB-694 is a fatty acid amide hydrolase (FAAH) inhibitor.

MDPD boosts AtFAAH, the enzyme degrading NAEs in Arabidopsis, reducing NAE 12:0's growth inhibition.

Potent FAAH inhibitor

Dual FAAH inhibitor/TRPV1 antagonist

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

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

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

anandamide transport inhibitor

MK-4409, a potent and selective fatty acid amide hydrolase (FAAH) inhibitor, is being investigated for the treatment of inflammatory and neuropathic pain.

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

JNJ-40355003 is a FAAH inhibitor that increases plasma levels of fatty acid amides in rats, dogs, and crabs.

AM 374 (HDSF), a fatty acid amide hydrolase (FAAH) inhibitor, demonstrates the capacity to inhibit amidase activity, boasting an IC50 value of 13 nM.

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].

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.

<p>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].</p>

FAAH/cPLA2α-IN-1 is a compound that simultaneously inhibits both FAAH and cPLA2α, demonstrating potent activity with half-maximal inhibitory concentrations (

OMDM-5 is a potent vanilloid receptor type 1 (TRPV1, EC50 = 75 nM) agonist, showing weak ligand activity at cannabinoid type 1 receptor (CB1, Ki=4.9 μM).

JP104 is an aryl carbamate that irreversibly inhibits fatty acid amide hydrolase (FAAH) with a pIC50 value of approximately 8 [1].

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

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

<p>MK-3168 (12C) functions as a FAAH inhibitor, exhibiting IC50 values of 1.0 nM, 5.5 nM, and 1.7 nM for human, rhesus, and rat respectively. It demonstrates effective brain uptake and FAAH-specific signaling. Additionally, 11 C MK-3168 is applicable as a FAAH PET tracer.</p>

<p>FAAH/MAGL-IN-1 (SIH 3) inhibits FAAH &amp; MAGL with IC50 of 31 &amp; 29 nM, useful in neuropathic pain research.</p>

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.

<p>AZ513 is a reversible FAAH inhibitor, exhibiting an IC50 of 551 nM for human FAAH and 27 nM for rat FAAH. It inhibits the hydrolysis of arachidonoyl ethanolamide in HEK293 cells transfected with human FAAH, with an IC50 of 360 nM.</p>

Sob-AM2 is an effective substrate targeting the fatty acid amide hydrolase (FAAH) expressed in the brain, with a Km of 1.3 μM. It delivers higher concentrations of Sobetirome to the central nervous system at minimal peripheral systemic doses, thereby activating the central thyroid hormone receptor β (TRβ).

FAAH/MAGL-IN-2: potent, reversible, oral FAAH & MAGL inhibitor, IC50: 11/36 nM, may research neuropathic pain, no locomotion issue.

<p>FAAH/MAGL-IN-3 irreversibly inhibits FAAH (IC50: 179 nM) &amp; MAGL (IC50: 759 nM) with low PAMPA permeability.</p>

<p>Dual FAAH/sEH-IN-1 inhibits both sEH (IC50: 9.6 nM) and FAAH (IC50: 7 nM), offering potent anti-inflammatory effects.</p>

TC-F 2 is a FAAH inhibitor.