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 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related FAAH Products |
|---|
| N-Benzyllinolenamide
N-Benzyllinolenamide is a natural macamide isolated from Lepidium meyenii, acts as an inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 41.8 μM. |
| N-(3-Methoxybenzyl)palmitamide
N-(3-Methoxybenzyl)Palmitamide is a promising inhibitor of FAAH for the treatment of pain, inflammation and CNS degenerative disorders. |
| VU534
VU534 is a NAPE-PLD agonist with an EC50 of 0.30 μM.In addition, VU534 can dependently enhance Efferocytosis in macrophages. VU534 can be used in studies of cardiometabolic diseases. |
| MK-4409
MK-4409 is a potent oxazole FAAH inhibitor and can be used for the research of inflammatory and neuropathic pain. |
| N-Benzylpalmitamide
N-Benzylpalmitamide is a macamide isolated from Lepidium meyenii, acts as an inhibitor of fatty acid amide hydrolase (FAAH). |
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