| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (219.08 mM), Sonication is recommended.
Ethanol : 22.8 mg/mL (49.95 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (8.76 mM), Sonication is recommended.
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| Keywords | sensation | PF-3845 | PF3845 | PF 3845 | pain | Inhibitor | inhibit | inflammation | hydrolase | Fatty acid amide hydrolase | fatty | FAAH | depression | Autophagy | anxiety | amide | acid |
| Inhibitors Related | Stavudine | Aceglutamide | Hemin | Tamoxifen | Cysteamine hydrochloride | Guanidine hydrochloride | Hydroxychloroquine | Enzalutamide | Paeonol | Naringin | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Antidepressant Compound Library | Anti-Obesity Compound Library | Autophagy Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library |
United States
