Chemical Name: 5-[[5-(2,8-Dimethyl-5H-dibenzo[a,d]cyclohepten-5-yl)-3,4-dihydro-2-oxo-4-thioxo-1(2H)-pyrimidinyl]methyl]-N-2H-tetrazol-5-yl-2-furancarboxamide
Biological ActivityAR-C 118925XX is a potent, selective, competitive and reversible P2Y2 receptor antagonist (pA2 = 8.43). Inactive against a panel of 37 other receptors at a concentration of 10 μM. AR-C 118925XX inhibits ATP-γS-induced mucin secretion in bronchial epithelial cells (IC50 = 1 μM). Inhibits P2Y2 receptor-induced β-arrestin translocation in vitro (pA2 = 37.2-51.3 nM).
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Synthesis, characterization, and in vitro evaluation of the selective P2Y2 receptor antagonist AR-C118925.
Rafehi et al.
Nucleotide-mediated mucin secretion from differentiated human bronchial epithelial cells.
Kemp et al.
Am.J.Respir.Cell Mol.Biol., 2004;31:446
The design of P2Y2 antagonists for the treatment of inflammatory diseases.
Abstract of papers, 224th ACS National Meeting, Boston, MA, 2002;
Citations for AR-C 118925XX
The citations listed below are publications that use Tocris products. Selected citations for AR-C 118925XX include:
7 Citations: Showing 1 - 7
Autocrine regulation of wound healing by ATP release and P2Y 2 receptor activation
Authors: McEwan Et al.
Life Sci 2021;283:119850
Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
Authors: Dosch Et al.
Characterisation of P2Y2 receptors in human vascular endothelial cells using AR-C118925XX, a competitive and selective P2Y2 antagonist.
Authors: Muoboghare Et al.
Br J Pharmacol 2019;176:2894
Adenosine triphosphate is co-secreted with glucagon-like peptide-1 to modulate intestinal enterocytes and afferent neurons.
Authors: Lu Et al.
Real-time scratch assay reveals mechanisms of early calcium signaling in breast cancer cells in response to wounding.
Authors: Pratt Et al.
P2Y2R-mediated inflammasome activation is involved in tumor progression in breast cancer cells and in radiotherapy-resistant breast cancer.
Authors: Jin Et al.
Int J Oncol 2018;53:1953
Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells.
Authors: Kleiner Et al.
Mol Vis 2018;24:647
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