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FAAH Inhibitors (inhibitors, agonists and modulators)
Fatty acid amide hydrolase or FAAH (oleamide hydrolase, anandamide amidohydrolase) is a member of the serine hydrolase family of enzymes. FAAH is an integral membrane hydrolase with a single N-terminal transmembrane domain. In vitro, FAAH has esterase and amidase activity. In vivo, FAAH is the principal catabolic enzyme for a class of bioactive lipids called the fatty acid amides (FAAs). www.bocsci.com
Arachidonyl serotonin - CAS 187947-37-1
Catalog Number: Molecular Weight: 462.67 Molecular Formula: C30H42N2O2 Description: Arachidonyl serotonin is a dual target agent of transient receptor potential vanilloid- type I (TRPV1) antagonist and fatty acid amide hydrolase (FAAH) inhibitor, which is responsible for inactivation of anandamide and other endogenous cannabinoids. Its IC50 values are 37-40 nM and 5.6 μM for TRPV1 and FAAH respectively. It inhibits the FAAH activity isolated from mouse
neuroblastoma cells with an IC50 value of 12 µM. It is a very tight binding, competitive inhibitor of FAAH. It does not inhibit cPLA2 and is essentially devoid of cannabimimetic activity. It was shown to be present in the ileum and jejunum of the gastrointestinal tract and modulate glucagon-like peptide-1 (GLP-1) secretion. It displays strong analgesic activity against both acute and chronic peripheral pain in rodents.
FAAH-IN-2 - CAS 184475-71-6
Catalog Number:184475-71-6 Molecular Weight: 319.72 Molecular Formula: C15H11ClFN3O2 Description: A metabolite of Gefitinib.
Biochanin A - CAS 491-80-5
Catalog Number: 491-80-5 Molecular Weight: 284.26 Molecular Formula: C16H12O5 Description: Biochanin A, an O-methylated isoflavone from Trifolium pratense, inhibits protein tyrosine kinase (PTK) of epidermal growth factor receptor with IC50 values of 91.5 μM.
PF 750 - CAS 959151-50-9
Catalog Number: Molecular Weight: 345.44 Molecular Formula: C22H23N3O Description: PF 750 is a potent, time-dependent, irreversible FAAH inhibitor (IC50 = 16.2 nM) that
exhibits no activity at a range of other serine hydrolases. Activity-based profiling of various human and murine tissue proteome samples revealed that PF-750 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 µM.
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URB597 - CAS 546141-08-6
Catalog Number: 546141-08-6 Molecular Weight: 338.4 Molecular Formula: C20H22N2O3 Description: URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets. Phase 1.
PDP-EA - CAS 861891-72-7
Catalog Number: Molecular Weight: 405.61 Molecular Formula: C25H43NO3
Description: PDP-EA, an activator of fatty acid amide hydrolase (FAAH) from plant and mammalian species, is a FAAH activator, which is proposed to enhance amidohydrolase activity of FAAH by reducing negative feedback mechanisms.
TC-F 2 - CAS 1304778-15-1
Catalog Number: Molecular Weight: 439.51 Molecular Formula: C26H25N5O2
Description: TC-F 2 is a potent, reversible and noncovalent inhibitor of fatty acid amide hydrolase (FAAH) (IC50 = 28 and 100 nM for human and rat FAAH, respectively).
TAK 21d - CAS 1143578-94-2
Catalog Number: Molecular Weight: 397.38 Molecular Formula: C19H17F2N7O Description: TAK 21d is a potent and brain penetrating FAAH inhibitor (IC50 = 0.28 and 0.72 nM at
rat and human FAAH, respectively). TAK 21d exhibits analgesic effects in vivo models of neuropathic and inflammatory pain.
SA 47 - CAS 792236-07-8
Catalog Number: Molecular Weight: 334.41 Molecular Formula: C17H26N4O3
Description: SA 47 is a selective fatty acid amide hydrolase (FAAH) inhibitor.
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SA 57 - CAS 1346169-63-8
Catalog Number: Molecular Weight: 338.83 Molecular Formula: C17H23ClN2O3
Description: SA 57 is a potent fatty acid amide hydrolase (FAAH) inhibitor (IC50 <10 nM), and also inhibits MAGL at higher concentrations (IC50 = 410 nM and 1.4 μM, respectively).
Palmitoylisopropylamide - CAS 189939-61-5
Catalog Number: Molecular Weight: 297.52 Molecular Formula: C19H39NO Palmitoyl-N-isopropylamide, a synthetic analog of palmitoyl ethanolamide, is an Description: inhibitor of the FAAH (fatty acid amide hydrolase); pIC50 = 4.89 for inhibition of [3H]-anandamide metabolism. It displays little binding to CB1 and CB2 receptors (IC50 > 100 μM) and very weakly blocks anandamide uptake (IC50 ~ 100 μM).
AM 1172 - CAS 251908-92-6
Catalog Number: Molecular Weight: 409.60 Molecular Formula: C27H39NO2
Description: AM 1172, an AEA analogue, has been found to be an anandamide uptake inhibitor as well as a cannabinoid receptor partial agonist.
PF-3845 - CAS 1196109-52-0
Catalog Number: 1196109-52-0 Molecular Weight: 456.469 Molecular Formula: C24H23F3N4O2 Description: PF-3845 is a potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM). It reduces inflammatory pain via a cannabinoid receptor-dependent mechanism.
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LY2183240 - CAS 874902-19-9
Catalog Number: 874902-19-9 Molecular Weight: 307.35 Molecular Formula: C17H17N5O Description: LY2183240 is a novel and highly potent blocker of anandamide uptake. It inhibits fatty acid amide hydrolase (FAAH) activity. It increases brain anandamide concentration and exerts antinociceptive effects in formalin model of pain.
PF-04457845 - CAS 1020315-31-4
Catalog Number: 1020315-31-4 Molecular Weight: 455.43 Molecular Formula: C23H20F3N5O2 Description: PF-04457845 is a potent and exquisitely selective inhibitor of FAAH, with an IC50 of 7.2 nM, and both analgesic and antiinflammatory effects in animal studies comparable to naproxen.
JZL195 - CAS 1210004-12-8
Catalog Number: 1210004-12-8 Molecular Weight: 433.46 Molecular Formula: C24H23N3O5 Description: JZL195 is a potent dual inhibitor of Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), enzymes that degrade the endocannabinoids 2-arachidonoylglycerol (2- AG) and anandamide (AEA), the endogenous ligands for the cannabinoid G-protein coupled receptors CB1 and CB2. IC50 values are 2 nM for MAGL and 4 nM for FAAH. JZL195 has been shown
to inhibit endocannabinoid hydrolysis and elevate 2-AG and AEA levels in vivo.
FAAH inhibitor 1 - CAS 326866-17-5
Catalog Number: 326866-17-5 Molecular Weight: 497.65 Molecular Formula: C24H23N3O3S3 Description: Time-dependent preincubation study of FAAH inhibitor 1 was consistent with it being a reversible inhibitor. Activity-based protein-profiling (ABPP) evaluation of FAAH inhibitors 1 in rat tissues revealed that it had exceptional selectivity and no off-target activity with respect to other serine hydrolases. Molecular shape overlay of FAAH inhibitor 1 with a known FAAH inhibitor indicated that these compounds might act as transitionstate analogues, forming putative
hydrogen bonds with catalytic residues and mimicking the charge distribution of the tetrahedral transition state. FAAH inhibitors 1 was exclusively specific against FAAH in rat brain and had no missing protein bands in all the other tissues that were tested.
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JNJ-42165279 - CAS 1346528-50-4
Catalog Number: 1346528-50-4 Molecular Weight: 410.81 Molecular Formula: C18H17ClF2N4O3 Description: JNJ-42165279 is a fatty acid amide hydrolase (FAAH) inhibitor developed by Janssen Pharmaceutica and IC50 value is 70 nM. It is described as a covalently binding but slowly reversible selective inhibitor of FAAH. Phase II human trials for the treatment of anxiety disorders and major depressive disorder is on-going.
BIA10-2474 - CAS 1233855-46-3
Catalog Number: 1233855-46-3 Molecular Weight: 300.36 Molecular Formula: C16H20N4O2 Description: This active molecular is a reversible FAAH (fatty acid amide hydrolase) inhibitor that increases levels of the neurotransmitter anandamide in the central nervous system and in peripheral tissues (except the brain and spinal cord) under the development of Bial-Portela & Ca.
SA. BIA 10-2474 can interact with the human endocannabinoid system and was inpplicated in the treatment of a range of different medical conditions including anxiety, Parkinson's disease, chronic pain of multiple sclerosis, cancer, hypertension and obesity. Clinical trial with BIA 10-2474 was on-going. However, severe adverse events occurred in January 2016 affecting 5 patients, including leading to the death of one.
JNJ-40355003 - CAS 1394894-41-7
Catalog Number: 1394894-41-7 Molecular Weight: 422.91 Molecular Formula: C23H23ClN4O2
Description: JNJ-40355003 is a selective fatty acid amide hydrolase (FAAH) inhibitor. JNJ- 40355003 can elevate the plasma levels of anandamide, oleoyl ethanolamide, and palmitoyl ethanolamide in animal model.
OL135 - CAS 681135-77-3
Catalog Number: 681135-77-3 Molecular Weight: 334.42 Molecular Formula: C21H22N2O2 Description: OL135 is a CNS penetrant, highly potent and selective reversible inhibitor of FAAH. It
exhibits analgesic pharmacology in various animal models without the motor impairment associated with direct CB1 agonism. It increases the analgesic and hypothermic activity of anandamide.
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