1. Metabolic Enzyme/Protease
    Neuronal Signaling
  2. FAAH

JNJ-42165279 

Cat. No.: HY-19636
Handling Instructions

JNJ-42165279 is a FAAH inhibitor with IC50 of 70 ± 8 nM and 313 ± 28 nM for hFAAH and rFAAH, respectively.

For research use only. We do not sell to patients.
JNJ-42165279 Chemical Structure

JNJ-42165279 Chemical Structure

CAS No. : 1346528-50-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $165 In-stock
5 mg $150 In-stock
10 mg $240 In-stock
50 mg $720 In-stock
100 mg $990 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

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Description

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]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02432703 Janssen Research & Development, LLC Phobic Disorders June 15, 2015 Phase 2
NCT02498392 Janssen Research & Development, LLC Depressive Disorder|Anxiety October 2015 Phase 2
NCT02065739 Janssen Pharmaceutica N.V., Belgium Healthy January 2014 Phase 1
NCT02169973 Janssen Research & Development, LLC Healthy February 2014 Phase 1
NCT01826786 Janssen Research & Development, LLC Healthy August 2013 Phase 1
NCT01964651 Janssen Research & Development, LLC Healthy October 2013 Phase 1
NCT01650597 Janssen-Cilag International NV Healthy Volunteers|Pharmacokinetics August 2011 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.4343 mL 12.1714 mL 24.3427 mL
5 mM 0.4869 mL 2.4343 mL 4.8685 mL
10 mM 0.2434 mL 1.2171 mL 2.4343 mL
References
Molecular Weight

410.8

Formula

C₁₈H₁₇ClF₂N₄O₃

CAS No.

1346528-50-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
JNJ-42165279
Cat. No.:
HY-19636
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