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PF-3845

Catalog No. T6043   CAS 1196109-52-0

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

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PF-3845 Chemical Structure
PF-3845, CAS 1196109-52-0
Pack Size Availability Price/USD Quantity
2 mg In stock $ 35.00
5 mg In stock $ 54.00
10 mg In stock $ 98.00
25 mg In stock $ 216.00
50 mg In stock $ 405.00
100 mg In stock $ 590.00
1 mL * 10 mM (in DMSO) In stock $ 54.00
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Purity: 99.58%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing 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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (219 mM)

Ethanol: 22.8 mg/mL (50 mM)

TargetMolReferences and Literature

1. Ahn K et al, Chem Biol, 2009,16(4), 411-20. 2. Booker L, et al, Br J Pharmacol, 2012, 165(8), 2485-2496.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Highly Selective Inhibitor Library NO PAINS Compound Library Anti-Obesity Compound Library Target-Focused Phenotypic Screening Library Antidepressant Compound Library Lipid Metabolism Compound Library Anti-Metabolism Disease Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max

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Keywords

PF-3845 1196109-52-0 Autophagy Metabolism Neuroscience FAAH Inhibitor PF 3845 inhibit depression hydrolase anxiety PF3845 Fatty acid amide hydrolase sensation pain fatty amide inflammation acid inhibitor

 

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