A-839977

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

413, 26

A Potent and Selective Antagonist of P2X7 Receptors

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

41116134

A-839977 is a potent and selective antagonist of P2X7 receptors, shown to inhibit BzATP-induced Ca2+ responses at human, rat and mouse P2X7 receptors with IC50 values of 20 nM, 42 nM and 150 nM, respectively. A-839977 produces significant anti-nociception and anti-hyperalgesia (ED50 = 40-100μMol/kg) in animal models of inflammatory pain1.

Yes

A-839977 is a potent and selective antagonist of the P2X7 receptor. It inhibits BzATP-induced Ca2+ responses of human, rat and mouse P2X7 receptors with IC50 values of 20 nM, 42 nM and 150 nM, respectively1.Selective P2X7 receptor antagonists, including A-839977, reduce inflammatory and neuropathic pain in animal models. In mice, A-839977 produces robust anti-hyperalgesia in a model of inflammatory pain.The P2X7 receptor is a member of the ligand-gated ion channels activated by extracellular ATP. There are seven receptor subtypes: P2X1-P2X7. P2X7 receptors participate in a variety of cellular responses such as membrane permeabilization, activation of caspases, cytokine release, cell proliferation, and apoptosis. P2X7 receptors are highly expressed throughout autonomic, sensory and central neurons and in visceral smooth muscle, immune cells and epithelia2, 3.