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JNJ-42165279 is a potent and selective FAAH inhibitor. JNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 exhibited excellent ADME and pharmacodynamic properties as evidenced by its ability to block FAAH in the brain and periphery of rats and thereby cause an elevation of the concentrations of anandamide, oleoylethanolamide and palmitoyl ethanolamide.
In vivo, JNJ-42165279 exhibits relatively rapid clearance in the course of rat pharmacokinetic experiments, manifesting as a low AUC and Cmax; however, sufficiently high exposures were obtainable to support preclinical animal models. In a subsequent higher dose (20 mg/kg) oral PK experiment, compound concentrations were determined both in the plasma and brain of rats.
| Molecular Weight | 410.8 |
| Formula | C18H17ClF2N4O3 |
| CAS Number | 1346528-50-4 |
| Solubility (25°C) | DMSO ≥ 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related FAAH Products |
|---|
| JNJ-1661010
JNJ-1661010 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. |
| URB597
URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets. |
| PF-3845
PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2. |
| Biochanin-A
Biochanin A is A naturally occurring fatty acid amide hydrolase (FAAH) inhibitor that inhibits FAAH in mice, rats and humans with FAAH IC50 of 1.8, 1.4 and 2.4 μM, respectively. |
| FAAH-IN-2
FAAH-IN-2 is a potent FAAH (fatty acid amide hydrolase) inhibitor. |
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