AR-C 118925XX
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
Purity: ≥97%
Biological Activity
AR-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).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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Background References
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Synthesis, characterization, and in vitro evaluation of the selective P2Y2 receptor antagonist AR-C118925.
Rafehi et al.
Purinergic.Signal., 2017;13:89 -
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.
Meghani
Abstract of papers, 224th ACS National Meeting, Boston, MA, 2002;
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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
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Autocrine regulation of wound healing by ATP release and P2Y 2 receptor activation
Authors: McEwan Et al.
Life Sci 2021;283:119850
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Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
Authors: Dosch Et al.
Elife 2019;8
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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
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Adenosine triphosphate is co-secreted with glucagon-like peptide-1 to modulate intestinal enterocytes and afferent neurons.
Authors: Lu Et al.
Nat.Commun. 2019;10:1029
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Real-time scratch assay reveals mechanisms of early calcium signaling in breast cancer cells in response to wounding.
Authors: Pratt Et al.
Oncotarget 2018;9:25008
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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
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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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