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

JNJ-42165279 

Cat. No.: HY-19636 Purity: 99.87%
COA 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

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Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 145 In-stock
Solid
5 mg USD 132 In-stock
10 mg USD 198 In-stock
25 mg USD 385 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

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

Appearance

Solid

Formula

C18H17ClF2N4O3

CAS No.
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 2 years
-20°C 1 year
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 available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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