PF-3845

SKU: orb1301124

Description

PF-3845 is a potent and selective irreversible inhibitor of fatty acid amide hydrolase (FAAH), exhibiting a Ki of 230 nM with minimal activity against FAAH2. It is widely used as a pharmacological tool in vitro and in vivo to investigate the endocannabinoid system, pain, and inflammation.

Research Area

Cell Biology, Metabolism Research, Neuroscience

Key Properties

• CAS Number: 1196109-52-0
• MW: 456.46
• Purity: 98.00% (May vary between batches)
• Formula: C₂₄H₂₃F₃N₄O₂
• SMILES: FC(F)(F)c1ccc(Oc2cccc(CC3CCN(CC3)C(=O)Nc3cccnc3)c2)nc1
• Target: Autophagy,FAAH
• Solubility: Ethanol:22.8 mg/mL (49.95 mM);DMSO:100 mg/mL (219.08 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.76 mM)

Bioactivity

• Target IC50:
  FAAH:230 nM(Ki)
• In Vivo:
  PF-3845 treated mice (10 mg/kg, i.p.) shows rapid and complete inactivation of FAAH in the brain, as judged by competitive activity-based protein profiling (ABPP) with the serine hydrolase-directed probe fluorophosphonate (FP)-rhodamine. PF-3845 shows a long duration of action up to 24 hour. PF-3845-treated mice also shows dramatic (>10-fold) elevation in brain levels of AEA and other NAEs (N-pamitoyl ethanolamine [PEA] and N-oleoyl ethanolamine [OEA]). FAAH is AEA-degrading enzyme fatty acid amide hydrolase. PF-3845 (1–30 mg/kg, oral administration [p.o.]) causes a dose dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg (rats are analyzed at 4 hour post dosing with PF-3845). At higher doses (10 and 30 mg/kg), PF-3845 inhibits pain responses to an equivalent, if not greater, degree than the nonsteroidal anti-inflammatory drug naproxen (10 mg/kg, p.o.). PF-3845 (10 mg/kg, i.p.) significantly reverses LPS-induced tactile allodynia, but doesn't modify paw withdrawal thresholds in the saline-injected paw.
• In Vitro:
  PF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

pain, inhibit, inflammation, Inhibitor, Fatty acid amide hydrolase, fatty, FAAH, hydrolase, depression, anxiety, amide, Autophagy, acid, PF-3845, PF3845, PF 3845, sensation

Compound Identifiers

PubChem CID

25154867