AR-C 118925XX

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Description: Selective and competitive P2Y2 antagonist
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% (HPLC)
Datasheet
Citations (15)
Reviews
Literature (1)

Biological Activity for AR-C 118925XX

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 for AR-C 118925XX

M. Wt 537.59
Formula C28H23N7O3S
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 216657-60-2
PubChem ID 54210200
InChI Key PVKNPGQAFNALOI-UHFFFAOYSA-N
Smiles CC(C=C1)=CC2=C1C(C3=CN(CC4=CC=C(C(NC5=NN=NN5)=O)O4)C(NC3=S)=O)C(C=CC(C)=C6)=C6C=C2

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.

Solubility Data for AR-C 118925XX

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 53.76 100

Preparing Stock Solutions for AR-C 118925XX

The following data is based on the product molecular weight 537.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.86 mL 9.3 mL 18.6 mL
5 mM 0.37 mL 1.86 mL 3.72 mL
10 mM 0.19 mL 0.93 mL 1.86 mL
50 mM 0.04 mL 0.19 mL 0.37 mL

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Product Datasheets for AR-C 118925XX

Certificate of Analysis / Product Datasheet
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References for AR-C 118925XX

References are publications that support the biological activity of the product.

Kemp et al (2004) Nucleotide-mediated mucin secretion from differentiated human bronchial epithelial cells. Am.J.Respir.Cell Mol.Biol. 31 446 PMID: 15231488

Meghani (2002) The design of P2Y2 antagonists for the treatment of inflammatory diseases. Abstract of papers, 224th ACS National Meeting, Boston, MA

Rafehi et al (2017) Synthesis, characterization, and in vitro evaluation of the selective P2Y2 receptor antagonist AR-C118925. Purinergic.Signal. 13 89 PMID: 27766552

Muoboghare et al (2019) Characterisation of P2Y2 receptors in human vascular endothelial cells using AR-C118925XX, a competitive and selective P2Y2 antagonist. Br.J.Pharmacol. 176 2894 PMID: 31116875


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Keywords: AR-C 118925XX, AR-C 118925XX supplier, AR-C118925XX, selective, competitive, purinergics, p2y2, antagonists, antagonises, inhibitors, inhibits, Purinergic, P2Y, Receptors, 4890, Tocris Bioscience

15 Citations for AR-C 118925XX

Citations are publications that use Tocris products. Selected citations for AR-C 118925XX include:

McEwan et al (2021) Autocrine regulation of wound healing by ATP release and P2Y 2 receptor activation Life Sci 283 119850 PMID: 34314735

Lawrence D et al (2021) Receptor-specific Ca2+ oscillation patterns mediated by differential regulation of P2Y purinergic receptors in rat hepatocytes. iScience 24 103139 PMID: 34646983

Brant E et al (2021) Endothelial pannexin 1-TRPV4 channel signaling lowers pulmonary arterial pressure in mice. Elife 10 PMID: 34490843

Timothy S et al (2021) Differential Regulation of ATP- and UTP-Evoked Prostaglandin E2 and IL-6 Production from Human Airway Epithelial Cells. J Immunol 207 1275-1287 PMID: 34389624

Muoboghare et al (2019) Characterisation of P2Y2 receptors in human vascular endothelial cells using AR-C118925XX, a competitive and selective P2Y2 antagonist. Br J Pharmacol 176 2894 PMID: 31116875

Tomohiro et al (2019) TRPC3-Nox2 axis mediates nutritional deficiency-induced cardiomyocyte atrophy. Sci Rep 9 9785 PMID: 31278358

Marc et al (2019) ATP amplifies NADPH-dependent and -independent neutrophil extracellular trap formation. Sci Rep 9 16556 PMID: 31719610

Ana C et al (2020) Vascular control of the CO2/H+-dependent drive to breathe. Elife 9 PMID: 32924935

Philip J et al (2020) Nucleotides released from palmitate-activated murine macrophages attract neutrophils. J Biol Chem 295 4902-4911 PMID: 32132172

Belinda L et al (2020) Pharmacological and genetic characterisation of the canine P2X4 receptor. Br J Pharmacol 177 2812-2829 PMID: 32017039

Pratt et al (2018) Real-time scratch assay reveals mechanisms of early calcium signaling in breast cancer cells in response to wounding. Oncotarget 9 25008 PMID: 29861849

Jin et al (2018) P2Y2R-mediated inflammasome activation is involved in tumor progression in breast cancer cells and in radiotherapy-resistant breast cancer. Int J Oncol 53 1953 PMID: 30226596

Kleiner et al (2018) Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells. Mol Vis 24 647 PMID: 30310263

Lu et al (2019) Adenosine triphosphate is co-secreted with glucagon-like peptide-1 to modulate intestinal enterocytes and afferent neurons. Nat.Commun. 10 1029 PMID: 30833673

Dosch et al (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife 8 PMID: 30735126


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


P2X and P2Y Receptors Scientific Review

P2X and P2Y Receptors Scientific Review

Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.