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PF-3845

SKU: orb1226827

Description

PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2.

Images & Validation

Key Properties

CAS Number1196109-52-0
MW456.46
Purity>98% (HPLC)
FormulaC??H??F?N?O?
SMILESO=C(N1CCC(CC2=CC=CC(OC3=NC=C(C(F)(F)F)C=C3)=C2)CC1)NC4=CC=CN=C4
TargetFAAH
SolubilityDMSO:45.7 mg/mL (100 mM);Ethanol:22.8 mg/mL (50 mM)

Bioactivity

In Vivo
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.
In Vitro
PF-3845 (0.5 nM-10 μM; 40 min) inhibits human FAAH-1 (IC50 = 18 nM) in a concentration-dependent manner, and shows negligible activity against FAAH-2 (IC50>10 μM) in COS-7 cells. PF-3845 (0.1-1000 μM; 48 h) significantly decreases the Colo-205 cell viability.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

PF3845 | PF-3845 | PF 3845

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Protocol Information

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