For research use only. We do not sell to patients.
JNJ-42165279
CAS No. : 1346528-50-4
Biological Activity：JNJ-42165279 is a FAAH inhibitor with IC50 of 70 ± 8 nM and 313 ± 28 nM for hFAAH and rFAAH, respectively.
IC50 value: 70 ± 8 nM (for hFAAH), 313 ± 28 nM (for rFAAH )
Target：FAAH
JNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 exhibits high selectivity against a panel of 50 receptors, enzymes, transporters, and ion-channels at 10 μM, at which concentration it does not produce >50% inhibition of binding to any of the targets. Fortunately, JNJ-42165279 also does not inhibit CYPS (1A2, 2C8, 2C9, 2C19, 2D6, 3A4) or hERG when tested at a 10 μM compound concentration. [1]
in vivo: JNJ-42165279 exhibits excellent ADME and pharmacodynamic properties as evidenced by its ability to block FAAH in the brain and periphery of rats and thereby cause an elevation of the concentrations of anandamide (AEA), oleoyl ethanolamide (OEA), and palmitoyl ethanolamide (PEA). The compound was also efficacious in the spinal nerve ligation (SNL) model of neuropathic pain. JNJ-42165279 exhibits relatively rapid clearance in the course of rat pharmacokinetic experiments, manifesting as a low AUC and Cmax; however, sufficiently high exposures were obtainable to support preclinical animal models. In a subsequent higher dose (20 mg/kg) oral PK experiment, compound concentrations were determined both in the plasma and brain of rats. [1]
Research Area：Neurological Disease
Targets：Autophagy|FAAH
Related Screening Libraries:Covalent Screening Library Plus;Drug Repurposing Compound Library Plus;Clinical Compound Library Plus;Bioactive Compound Library Plus;Metabolism/Protease Compound Library;Neuronal Signaling Compound Library;Clinical Compound Library;Autophagy Compound Library;Drug Repurposing Compound Library;Covalent Screening Library;Anti-COVID-19 Compound Library;Lipid Metabolism Compound Library ;
Related Small Molecules:JNJ-1661010;MK-4409;JZL195;Carpro-AM1;FAAH-IN-6;SSR411298;FAAH inhibitor 1;N-Arachidonoylserotonin;Biochanin A;WWL154;PF-3845;SA72;N-Benzyllinolenamide;FAAH-IN-2;FP-Biotin;FAAH-IN-5;LY2183240;FAAH-IN-7;FAAH/MAGL-IN-2;SA 47;SA57;FAAH/MAGL-IN-1;FAAH/MAGL-IN-4;N-Benzyloleamide;URB937;URB-597
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
About Us:
- MedChemExpress (MCE) offers a wide range of high-quality research chemicals and biochemicals (novel life-science reagents, reference compounds and natural compounds) for scientific use；
- Structurally and synthetically diverse biologically active compounds；
- roduct quality is the key to our success and we take pride in offering only the highest-grade products.；
- We provide HNMR, LC-MS, HPLC, stability testing and activity assays of our products to clients.；
- Product identity, quality, purity and activity are assured by our robust quality control programs and procedures.；
- Customized order volume ranging from milligrams to kilograms scale；
Structurally and synthetically diverse biologically active compounds；
We provide customer-oriented services. To explore more, please contact us at [email protected]. Our team will gladly assist you.
