AR-C 118925XX

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Cat.No. 4890 - AR-C 118925XX | C28H23N7O3S | CAS No. 216657-60-2
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 (5)
Reviews
Literature

Biological Activity

Selective, competitive P2Y2 receptor antagonist. Inactive against a panel of 37 other receptors at a concentration of 10 μM. 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

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

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

Preparing Stock Solutions

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.

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

Certificate of Analysis / Product Datasheet
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References

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


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

5 Citations for AR-C 118925XX

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

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

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


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Literature in this Area

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