Molecular Formula | C24H23F3N4O2
|
Molar Mass | 456.46 |
Density | 1.323±0.06 g/cm3(Predicted) |
Boling Point | 623.6±55.0 °C(Predicted) |
Solubility | Soluble in DMSO (100 mM), ethanol (~20 mg/ml), DMF (~20 mg/ml), 1:3 EtOH:PBS(pH 7.2) ( |
Appearance | White to Brown Powder |
Color | white to tan |
pKa | 14.14±0.40(Predicted) |
Storage Condition | 2-8°C |
MDL | MFCD21365072 |
Use | A selective fatty acid amide hydrolase (FAAH) inhibitor. |
In vitro study | PF-3845 (0.5 nM-10 μM; 40 min) inhibits human FAAH-1 (IC 50 =18 nM) in a concentration-dependent manner, and shows negligible activity against FAAH-2 (IC 50 >10 μM) in COS-7 cells. PF-3845 (0.1-1000 μM; 48 h) significantly decreases the Colo-205 cell viability. |
In vivo study | PF-3845 (1-30 mg/kg; p.o.) produces cannabinoid receptor-dependent reductions in inflammatory pain in rat. PF-3845 (10 mg/kg; a single i.p.) selectively inhibits FAAH in mice for up to 24 hours. PF-3845 (10 mg/kg; a single i.p.) causes a dramatic and sustained elevation in Anandamide (AEA) in mice. Animal Model: Male Sprague-Dawley rats (200g- 250g) are injected CFA Dosage: 1, 3, 10, 30 mg/kg Administration: Oral administration Result: Caused a dose-dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg. |