A-839977

A-389977 is an antagonist of the purinergic P2X7 receptor. 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-1beta 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.Formal Name: 1-(2,3-dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]methyl]-1H-tetrazol-5-amine. CAS Number: 870061-27-1. Molecular Formula: C19H14Cl2N6O. Formula Weight: 413.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble. SMILES: ClC1=CC=CC(N2C(NCC3=CC=CC=C3OC4=CC=CC=N4)=NN=N2)=C1Cl. InChi Code: InChI=1S/C19H14Cl2N6O/c20-14-7-5-8-15(18(14)21)27-19(24-25-26-27)23-12-13-6-1-2-9-16(13)28-17-10-3-4-11-22-17/h1-11H,12H2,(H,23,24,26). InChi Key: GMVNBKZQJFRFAR-UHFFFAOYSA-N.