JNJ-54166060

Non Antibodies

P2X7 receptors

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

438, 81

A Novel Potent and Selective Antagonist of P2X7 Receptors

Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).

41116134

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.

Yes

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.