PF-3845 is a potent, selective, and irreversible fatty acid amide hydrolase (FAAH) inhibitor with a Ki of 0.23 μM. Fatty acid amide hydrolase (FAAH) is an enzyme that catalyzes N-acyl ethanolamines (NAEs), including the endocannabinoid arachidonoyl ethanolamide (AEA). Mechanistic and structural studies demonstrated that PF-3845 acts as a covalent inhibitor and carbamylates the active site serine241 of FAAH. PF-3845 covalently binds FAAH on Ser241 at the catalytic site, resulting in prolonged elevation of AEA in the brain and plasma in rats after treatment. Initial experiments indicated that PF-3845 is 10 to 20 times more potent than other FAAH inhibitors and has superior pharmacokinetic properties. PF-3845 significantly and persistently blockes inflammatory pain in rats through a cannabinoid receptor-dependent mechanism. In animal studies, PF-3845 elevated brain anandamide levels for up to 24 hours and produced a marked cannabinoid receptor-dependent reduction in inflammatory pain.
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| Animal models | Male C57BL/6 mice |
| Formulation | PF-3845 is dissolved at 1 mg/ml by sonication and vortexing directly into a solution of 18:1:1 v/v/v saline:emulphor:ethanol. |
| Dosages | 10 mg/kg or 1-30 mg/kg |
| Administration | Administered via i.p. 1 hour before sacrificed by CO2 or oral administration. |
| Molecular Weight | 456.46 |
| Formula | C24H23F3N4O2 |
| CAS Number | 1196109-52-0 |
| Solubility (25°C) | DMSO 90 mg/mL |
| 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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