| Name | PF-3845 |
| Description | PF-3845 is a potent, selective, and irreversible FAAH inhibitor with a Ki of 230 nM, exhibiting negligible activity against FAAH2. |
| 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] |
| 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)
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| Keywords | PF-3845 | Inhibitor | PF 3845 | Autophagy | inhibit | depression | hydrolase | anxiety | PF3845 | FAAH | Fatty acid amide hydrolase | sensation | pain | fatty | amide | inflammation | acid |
| Inhibitors Related | Stavudine | Xylitol | Myricetin | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Pain-Related Compound Library | Bioactive Compound Library | Antidepressant Compound Library | Inhibitor Library | Metabolism Compound Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Metabolism Disease Compound Library |
United States
