rfaah

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

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).

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.

5-HT6R/FAAH modulator 1 is a selective ligand for the serotonin 5-HT6 receptor and an inhibitor of the fatty acid amide hydrolase (FAAH). It exhibits a pKi of 6.33 for 5-HT6 and a pIC50 of 6.33 for FAAH. This compound also shows mild inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with a pIC50 of 5.12. Additionally, it can inhibit apoptosis and reduce reactive oxygen species (ROS) levels. 5-HT6R/FAAH modulator 1 is applicable in the study of neurological disorders such as Alzheimer's disease (AD).

CB2R/FAAH modulator-2 (compound 26) is a dual modulator targeting CB2R and FAAH, acting as a CB2R agonist (Ki = 10.8 nM) and FAAH inhibitor (IC50 = 6.2 μM), with a Ki value of 152.9 nM for CB1R. It has research value in cancer, deleterious inflammatory cascades in neurodegenerative diseases, and COVID-19 infection.

CB2R/FAAH modulator-3 (compound 27) is a modulator targeting CB2R and FAAH, acting as a CB2R agonist with a Ki value of 20.1 nM and a CB1R agonist with a Ki value of 67.6 nM, while inhibiting FAAH with an IC50 value of 3.4 μM. This compound has research value in cancer, neurodegenerative disease-related inflammatory cascades, and COVID-19 infection.

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