FAAH Inhibitor

Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH with IC₅₀s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.

Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC₅₀s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively.

Carmofur (HCFU) is a rat recombinant acid ceramidase inhibitor with an IC₅₀ of 29 nM. Carmofur is also a protease inhibitor of SARS-CoV-2 main protease (Mpro), fatty acid amide hydrolase (FAAH) and N-acylethanolamine acid amidase (NAAA). Carmofur has anti-cancer, anti-inflammatory and anti-virus activities, and can be used for the study of COVID-19 and acute lung injury (ALI).

URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC₅₀s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity.

CAY10499 (MAGL-IN-5) is a non-selective lipase inhibitor with IC₅₀ values of 144 nM and 14 nM for monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), respectively. Additionally, CAY10499 exhibits anti-inflammatory and antiviral activities.

5-HT6R/FAAH modulator 2 is a dual 5-HT6R antagonist and FAAH inhibitor with human 5-HT6R pK_i 7.24, human FAAH pIC₅₀ 5.47, and blood-brain barrier penetration.5-HT6R/FAAH modulator 2 modulates serotonergic signaling, blocks 5-HT6R function, inhibits endocannabinoid degradation via FAAH catalytic activity suppression.5-HT6R/FAAH modulator 2 exhibits neuroprotective effects against mitochondrial dysfunction, amyloid-β, and glutamate-induced toxicity, reverses memory deficits.5-HT6R/FAAH modulator 2 shows reduced cytotoxicity relative to oxygen-containing lead compounds.5-HT6R/FAAH modulator 2 can be used for the research of Alzheimer's disease.

FAAH-IN-10 is a FAAH inhibitor and TRPV1 antagonist, with an IC₅₀ of 0.57 μM against human FAAH. FAAH-IN-10 regulates FAAH activity, antagonizes TRPV1 activity, and exhibits analgesic and anti-inflammatory activities. FAAH-IN-10 does not induce TRPV1-mediated hyperthermia. FAAH-IN-10 can be used for pain-related research.

SRP-001 is an orally active, blood-brain barrier-permeable analgesic and antipyretic agent. SRP-001 reduces the expression level of FAAH, mildly inhibits hERG currents, generates AM404 (HY-101388), and maintains the integrity of hepatic tight junctions. SRP-001 exerts analgesic, antipyretic, and antinociceptive effects.

Redafamdastat (PF-04457845), a chemical probe, is a highly efficacious and selective FAAH inhibitor with IC₅₀ values is 7.2±0.63 nM and 7.4±0.62 nM for hFAAH and rFAAH, respectively.

PF-3845 is a potent, selective, irreversible and orally active inhibitor of fatty acid amide hydrolase (FAAH), with a K_i of 0.23 μM. PF-3845 is a covalent inhibitor that carbamylates FAAH's serine nucleophile. PF-3845 can reduce pain sensation, inflammation, and anxiety/depression without substantial effects on motility or cognition.

JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibitor with IC₅₀s of 2 and 4 nM, respectively.

LY2183240 is a highly potent blocker of anandamide uptake (IC₅₀= 270 pM; K_i=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC₅₀ of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC₅₀s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .

Oleoyl ethyl amide (N-Ethyloleamide) is a fatty acid amide hydrolase (FAAH) inhibitor. Oleoyl ethyl amide can counteract bladder overactivity.

URB937 is an orally active and peripherally restricted FAAH inhibitor (IC₅₀=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier).

JNJ-42165279 is an orally active FAAH inhibitor, with IC₅₀ values of 70 nM for hFAAH and 313 nM for rFAAH. JNJ-42165279 can be used in research related to the field of neuropathic pain.

VU534 is a NAPE-PLD activator, with an EC₅₀ of 0.30 μM. VU534 is dual inhibitors of FAAH and sEH (IC₅₀ of 1.2 μM). VU534 increases efferocytosis in a NAPE-PLD dependent manner. VU534 has the potential for cardiometabolic diseases study ^[1] .

Macamide B (N-Benzylhexadecanamide; Macamide 1) is a macamide isolated from Lepidium meyenii, acts as an inhibitor of fatty acid amide hydrolase (FAAH).

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC₅₀ values of 50 to 70mg/kg in various rat brain regions.

TC-F2 is a reversible non-covalent binding inhibitor of fatty acid amide hydrolase (FAAH) with an IC₅₀ of 28 nM. FAAH is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders.

1-Monomyristin acts as an insecticide, enzyme inhibitor, antibacterial and antifungal agent, with an IC₅₀ of 18 μM against rat FAAH and an IC₅₀ of 32 μM against rat MAGL. 1-Monomyristin inhibits 2-oleoylglycerol hydrolysis via MAGL. 1-Monomyristin suppresses the growth of Staphylococcus aureus, Aggregatibacter actinomycetemcomitans and Candida albicans. 1-Monomyristin is lethal to brine shrimp. 1-Monomyristin exhibits marginal cytotoxicity against prostate cancer cells. 1-Monomyristin is applicable to research related to bacterial infections, fungal infections, renal cancer, prostate adenocarcinoma and pancreatic cancer.