Home / P2Y Receptor Antagonists / AR-C 118925XX

AR-C 118925XX

Catalog #: 4890
15 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4890/5
AR-C 118925XX | CAS No. 216657-60-2 | P2Y Receptor Antagonists
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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%

Product Details
Citations (15)
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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

M.Wt:
537.59
Formula:
C28H23N7O3S
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥97%
Storage:
Store at -20°C
CAS No:
216657-60-2

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.

Background References

  1. Synthesis, characterization, and in vitro evaluation of the selective P2Y2 receptor antagonist AR-C118925.
    Rafehi et al.
    Purinergic.Signal., 2017;13:89
  2. Nucleotide-mediated mucin secretion from differentiated human bronchial epithelial cells.
    Kemp et al.
    Am.J.Respir.Cell Mol.Biol., 2004;31:446
  3. The design of P2Y2 antagonists for the treatment of inflammatory diseases.
    Meghani
    Abstract of papers, 224th ACS National Meeting, Boston, MA, 2002;
  4. Adenosine triphosphate is co-secreted with glucagon-like peptide-1 to modulate intestinal enterocytes and afferent neurons
    VB Lu, J Rievaj, EA O'Flaherty, CA Smith, R Pais, LA Pattison, G Tolhurst, AB Leiter, DC Bulmer, FM Gribble, F Reimann
    Nat Commun, 2019;10(1):1029.
  5. Macrophage centripetal migration drives spontaneous healing process after spinal cord injury
    K Kobayakawa, Y Ohkawa, S Yoshizaki, T Tamaru, T Saito, K Kijima, K Yokota, M Hara, K Kubota, Y Matsumoto, K Harimaya, K Ozato, T Masuda, M Tsuda, T Tamura, K Inoue, VR Edgerton, Y Iwamoto, Y Nakashima, S Okada
    Sci Adv, 2019;5(5):eaav5086.

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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:

15 Citations: Showing 1 - 10

  1. Autocrine regulation of wound healing by ATP release and P2Y 2 receptor activation
    Authors: McEwan Et al.
    Life Sci  2021;283:119850
  2. Receptor-specific Ca2+ oscillation patterns mediated by differential regulation of P2Y purinergic receptors in rat hepatocytes.
    Authors: Lawrence D Et al.
    iScience  2021;24:103139
  3. Differential Regulation of ATP- and UTP-Evoked Prostaglandin E2 and IL-6 Production from Human Airway Epithelial Cells.
    Authors: Timothy S Et al.
    J Immunol  2021;207:1275-1287
  4. Endothelial pannexin 1-TRPV4 channel signaling lowers pulmonary arterial pressure in mice.
    Authors: Brant E Et al.
    Elife  2021;10
  5. Vascular control of the CO2/H+-dependent drive to breathe.
    Authors: Ana C Et al.
    Elife  2020;9
  6. Nucleotides released from palmitate-activated murine macrophages attract neutrophils.
    Authors: Philip J Et al.
    J Biol Chem  2020;295:4902-4911
  7. Pharmacological and genetic characterisation of the canine P2X4 receptor.
    Authors: Belinda L Et al.
    Br J Pharmacol  2020;177:2812-2829
  8. TRPC3-Nox2 axis mediates nutritional deficiency-induced cardiomyocyte atrophy.
    Authors: Tomohiro Et al.
    Sci Rep  2019;9:9785
  9. ATP amplifies NADPH-dependent and -independent neutrophil extracellular trap formation.
    Authors: Marc Et al.
    Sci Rep  2019;9:16556
  10. Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
    Authors: Dosch Et al.
    Elife  2019;8

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