FAAH

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

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

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

Dual FAAH inhibitor/TRPV1 antagonist

FAAH inhibitor 1 (Benzothiazole analog 3) is an effective 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.

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

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

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].

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

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

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.

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].

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.

NRMA-8 is a small-molecule nuclear receptor modulator capable of penetrating the brain. It holds potential for research into central nervous system (CNS) diseases, including Alzheimer's disease, Parkinson's disease, demyelinating diseases, and glioblastoma.

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-1 (SIH 3) inhibits FAAH & MAGL with IC50 of 31 & 29 nM, useful in neuropathic pain research.

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.