Every lot is tried & tested in a relevant biological assay.
- Swanson, D.M. et al. (2016) J. Med. Chem. 59, 8535.
- 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.
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.
JNJ-54166060 (#J-125) is a highly pure, synthetic, and biologically active compound.
- Anti-P2X7 Receptor Antibody (#APR-004)
- Anti-P2X7 Receptor (extracellular) Antibody (#APR-008)
- Anti-P2X7 Receptor (extracellular)-ATTO Fluor-633 Antibody (#APR-008-FR)
- Anti-P2X7 Receptor (extracellular)-ATTO Fluor-488 Antibody (#APR-008-AG)
- Anti-P2X7 Receptor (extracellular)-FITC Antibody (#APR-008-F)
- Anti-P2X7 Receptor-ATTO Fluor-550 Antibody (#APR-004-AO)
- HMA (#H-130)
- Chelerythrine chloride (#C-400)
- AACBA hydrochloride (#A-410)
- AZ 10606120 dihydrochloride (#A-405)
- A-804598 (#A-415)
- A-740003 (#A-420)
- AZD-9056 hydrochloride (#A-425)
- ZINC9315614 (#Z-145)
- A-839977 (#A-470)
- AZ11645373 (#A-395)
- ZINC58368839 (#Z-135)
- GW 791343 hydrochloride (#G-115)
- JNJ-47965567 (#J-115)
- KN-62 (#K-120)
- CAY10593 (VU0155069) (#C-385)
- Garcinolic acid (#G-155)
- BzATP triethylammonium salt (#A-385)