1. Metabolic Enzyme/Protease
    Neuronal Signaling
    Autophagy
  2. FAAH
    Autophagy
  3. JNJ-42165279

JNJ-42165279 

Cat. No.: HY-19636 Purity: 99.97%
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 USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 288 In-stock
Estimated Time of Arrival: December 31
50 mg USD 864 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1188 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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
Molecular Weight

410.80

Formula

C₁₈H₁₇ClF₂N₄O₃

CAS No.

1346528-50-4

SMILES

O=C(N1CCN(CC2=CC=C(OC(F)(F)O3)C3=C2)CC1)NC4=C(Cl)C=CN=C4

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (243.43 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (7.30 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3 mg/mL (7.30 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (7.30 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
JNJ-42165279
Cat. No.:
HY-19636
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