Formulation: A crystalline solid
Formal Name: 1-(2,3-dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]methyl]-1H-tetrazol-5-amine
Purity: ≥98%
Formula Markup: C19H14Cl2N6O
Formula Weight: 413,3
Shelf life (days): 1460
CAS Number: 870061-27-1
Notes: A-389977 is an antagonist of the purinergic P2X7 receptor.{57152} It inhibits BzATP-evoked intracellular calcium influx in 1321N1 cells expressing human, rat, and mouse receptors (IC50s = 20, 42, and 150 nM, respectively). A-839977 inhibits BzATP-induced YO-PRO dye uptake, a marker of membrane pore formation, and IL-1β release from THP-1 cells (IC50s = 6.6 and 37 nM, respectively). In vivo, A-389977 (30, 100, and 300 µmol/kg, i.p.) reduces thermal hyperalgesia in rats. A-389977 (40 mg/kg) reduces thermal and mechanical hyperalgesia in a rat MRMT-1 mammary carcinoma model of cancer-induced bone pain.{57151}