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PF-3845 is a potent, selective, and irreversible FAAH inhibitor with a Ki of 230 nM, exhibiting negligible activity against FAAH2.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | 33 € | In Stock | |
5 mg | 51 € | In Stock | |
10 mg | 93 € | In Stock | |
25 mg | 205 € | In Stock | |
50 mg | 384 € | In Stock | |
100 mg | 560 € | In Stock | |
1 mL x 10 mM (in DMSO) | 51 € | In Stock |
Description | PF-3845 is a potent, selective, and irreversible FAAH inhibitor with a Ki of 230 nM, exhibiting negligible activity against FAAH2. |
Targets&IC50 | FAAH:230 nM(Ki) |
In vitro | PF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile. [1] |
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.). [1] 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. [2] |
Molecular Weight | 456.46 |
Formula | C24H23F3N4O2 |
Cas No. | 1196109-52-0 |
Smiles | FC(F)(F)c1ccc(Oc2cccc(CC3CCN(CC3)C(=O)Nc3cccnc3)c2)nc1 |
Relative Density. | 1.323 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (219 mM) Ethanol: 22.8 mg/mL (50 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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