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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 |
| 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. |
| 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. |
| PF 04457845
PF 04457845 is a potent and selective irreversible FAAH inhibitor. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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