Overview
Alternative Name (R)‑(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro‑1H‑imidazo[4,5‑c]pyridine-5(4H)‑yl)methanone
Lyophilized Powder yes
Source Synthetic
MW: 438.81
Purity: >99% (HPLC)
Effective concentration 10 nM – 1 µM.
Structure
Chemical name (R)‑(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro‑1H‑imidazo[4,5‑c]pyridine-5(4H)‑yl)methanone.
Molecular formula C20F4H15N4OCl.
Activity JNJ-54166060 is a novel, potent and selective antagonist of purinergic P2X7 receptors, with IC50 of 4 nM on human receptors. Orally bioavailable, with an ED50 of 2.3 mg/kg and a brain/plasma ratio of close to 3 in rats1.
References-Activity
- Swanson, D.M. et al. (2016) J. Med. Chem. 59, 8535.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).
Storage of solutions -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
Our bioassay
Alomone Labs JNJ-54166060 inhibits human P2X7 receptors expressed in HEK-293 cells.Dose response curve of hP2X7 inhibition by JNJ-54166060 (#J-125). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of JNJ-54166060, and stimulated with 80 µM BzATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated at 65.6 nM.
Scientific background
JNJ-54166060 is a potent and selective antagonist of P2X7 receptors, displaying IC50 values of 4 nM for human P2X71. JNJ-54166060 has a high oral bioavailability with low-moderate clearance in preclinical species, and acceptable safety margins in rats1.
P2X receptors are a family of ion channels gated by ATP, a ubiquitous energy donor and receptor ligand in living cells. P2X receptors are ubiquitously expressed, including expression in neuronal, muscular, epithelial and immune cells and play a pivotal role in models of various pain conditions. P2X7 is responsible for mediating the release of proinflammatory cytokines known to have roles in inflammatory/immune conditions and pain2,3.
Target P2X7 receptors
Lyophilized Powder
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
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