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FAAH Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S2631 URB597 URB597 (KDS-4103) is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets. Phase 1.
International Journal of Nanomedicine, May 27, 2021, 3661-3678
Exp Cell Res, 2025, 449(2):114602
International Journal of Molecular Sciences, 2024, 12044
S2666 PF-3845 PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2.
Journal of Biological Chemistry, 2021 Jan, 100257
eLife, 2020, e55211
Elife, 2020, 9;9:e55211
S2377 Biochanin A Biochanin A (4-Methylgenistein), an O-methylated isoflavone from Trifolium pratense, inhibits protein tyrosine kinase (PTK) of epidermal growth factor receptor with IC50 values of 91.5 μM.
Frontiers in Oncology, July 08 2021, 652008
Mol Neurobiol, 2022, 10.1007/s12035-021-02674-6
Front Oncol, 2021, 11:652008
S2421 PF-04457845 PF-04457845 (PF-4457845) is a potent, favorable selective inhibitor of Fatty acid amide hydrolase (FAAH) with IC50 of 7.2 nM and 7.4 nM for hFAAH and rFAAH, respectively. This compound covalently modifies the active-site serine nucleophile of FAAH with exquisite selectivity relative to other members of the serine hydrolase superfamily.
The FASEB Journal, 2023, e22690
Journal of Biological Chemistry, 2021 Jan, 100257
Front Chem, 2018, 6:441
S0497 JNJ-42165279 JNJ-42165279 (JNJ-5279) is an inhibitor of fatty acid amide hydrolase (FAAH) that inhibits recombinant human and rat FAAH with IC50 of 70 nM and 313 nM, respectively.
Cell Death Differ, 2022, 10.1038/s41418-022-01054-4
S5329 FAAH-IN-2 FAAH-IN-2 is an inhibitor of fatty acid amide hydrolase (FAAH).
S6609 JZL195 JZL195 is a potent inhibitor of both FAAH and MAGL with IC50s of 2 and 4 nM respectively.
S3586 URB937 URB937 is an orally active and peripherally restricted FAAH inhibitor with IC50 of 26.8 nM and increases anandamide levels.
S2828 JNJ-1661010 JNJ-1661010 (Takeda-25) is a potent and selective FAAH inhibitor with IC50 of 10 nM (rat) and 12 nM (human), exhibits >100-fold selectivity for FAAH-1 when compared to FAAH-2.
S5932 BIA 10-2474 BIA 10-2474 is a novel fatty acid amide hydrolase (FAAH) inhibitor, with a potent inhibitory effect upon FAAH and prolonged action in vivo.
S8052 LY-2183240 LY-2183240 is a potent, covalent inhibitor of the EC-degrading enzyme fatty acid amide hydrolase (FAAH). This compound disrupts the cellular uptake of the lipid endocannabinoid (EC) anandamide and promote analgesia in vivo. It is also an inhibitor of monoacylgylcerol lipase (MGL).