FAAH Inhibitor

VDM11 is a potent and selective anandamide membrane transporter (AMT) inhibitor. VDM11 inhibits FAAH and MAGL and may act as an alternative FAAH substrate.

Carprofen (Standard) is the analytical standard of Carprofen. This product is intended for research and analytical applications. 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.

Eicosapentaenoyl serotonin (EPA-5-HT) is an endogenous fatty acid-serotonin conjugate lipid mediator. Eicosapentaenoyl serotonin acts as an inhibitor of fatty acid amide hydrolase (FAAH). Eicosapentaenoyl serotonin suppresses IL-17 release in Concanavalin A (HY-P2149)-stimulated human peripheral blood mononuclear cells. Eicosapentaenoyl serotonin is regulated by polyunsaturated fatty acids and modulates intestinal immunity and Th17 signaling. Eicosapentaenoyl serotonin can be used for the study of inflammatory bowel disease-related mechanisms.

ASP 8477 is an orally active and selective fatty acid amide hydrolase (FAAH) inhibitor with IC₅₀ values ​​of 3.99, 1.65, and 57.3 nM for human FAAH-1, FAAH-1 (P129T), and FAAH-2, respectively. ASP 8477 has central nervous system activity and can be used in analgesia research.

PF-622 is a selective FAAH inhibitor, and can be used for study of analgesic and anxiolytic/antidepressant.

FAAH/MAGL-IN-3 (Compound 10) is an irreversible fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) dual inhibitor with IC₅₀ values of 179 and 759 nM against FAAH and MAGL, respectively. FAAH/MAGL-IN-3 shows low PAMPA (Parallel Artificial Membrane Permeability Assay) permeability.

Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoid receptor (CB1) and inhibits FAAH with similar potencies (IC₅₀ = 2 nM).

FAAH/TRPV1 blocker-1 (compound 2R) is a dual FAAH/TRPV1 blocker, with IC₅₀ of 0.12 and 94.9 μM, respectively. FAAH/TRPV1 blocker-1 plays an important role in analgesic and anti-inflammatory research.

5-HT6R/FAAH modulator 1 is a selective serotonin 5-HT6 receptor ligand and the fatty acid amide hydrolase (FAAH) enzyme inhibitor. 5-HT6R/FAAH modulator 1 shows a pK_i of 6.33 (5-HT6) and a pIC₅₀ valuesof 6.29 (FAAH). 5-HT6R/FAAH modulator 1 also slightly inhibits acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) enzymes (pIC₅₀ = 5.12). 5-HT6R/FAAH modulator 1 can inhibit apoptosis and reduce ROS levels. 5-HT6R/FAAH modulator 1 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

3-Decyl-5,5'-diphenyl-2-thioxo-4-imidazolidinone (compound 45) is a potential inhibitor of fatty acid amide hydrolase (FAAH) (pI50: 5.89) and is active against CB(1) and CB(2) ) Lack of affinity for cannabinoid receptors.

Dual FAAH/sEH-IN-1 (compound 3) is a high affinity dual sEH (soluble epoxide hydrolase) and FAAH (fatty acid amide hydrolase) inhibitor, with IC₅₀ values of 9.6 and 7 nM, respectively. Dual FAAH/sEH-IN-1 shows antinociception against the inflammatory phase.

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/cPLA2α-IN-1 is a dual inhibitor of FAAH and cPLA2α with IC₅₀s of 32 and 47 nM, respectively.

Acetylhydrolase-IN-1 is a 1-Alkyl-2-acetylglycerophosphocholine esterase (Alkylacetyl-GPC: acetylhydrolase) inhibtor.

FAAH/MAGL-IN-1 (compound SIH 3) is a potent FAAH and MAGL inhibitor with IC₅₀s of 31 nM and 29 nM, respectively. FAAH/MAGL-IN-1 has the potential for the research of neuropathic pain.

SA57 is a potent, selective FAAH inhibitor with IC₅₀s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC₅₀s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC₅₀ of 850 nM), but not other brain serine hydrolases.

Carprofen-d₃ is the deuterium labeled Carprofen. 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.

FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC₅₀s of 11 nM and 36 nM (K_is of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to research neuropathic pain without causing locomotion impairment.

CB2R/FAAH modulator-2 (compound 26) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The K_i values for CB2R/FAAH modulator-2 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 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.

FAAH-IN-7 is a reversible and potent FAAH inhibitor with an IC₅₀ value of 8.29 nM. FAAH-IN-7 suppresses oxidative stress in 1321N1 astrocytes and exhibits notable neuroprotective effect in ex vivo neuroinflammation model.