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JNJ-42165279

Cat. No. M8950
JNJ-42165279 Structure
Size Price Availability Quantity
5mg USD 180 In stock
10mg USD 280 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

JNJ-42165279 is a potent and selective FAAH inhibitor. JNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 exhibited 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, oleoylethanolamide and palmitoyl ethanolamide.

In vivo, 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 410.8
Formula C18H17ClF2N4O3
CAS Number 1346528-50-4
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

Preclinical Characterization of the FAAH Inhibitor JNJ-42165279.
Keith JM, et al. ACS Med Chem Lett. 2015 Nov 2;6(12):1204-8. PMID: 26713105.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: JNJ-42165279 supplier, FAAH, inhibitors

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