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CGS 15943

Catalog #: 1699
7 Citations Datasheet / COA / SDS
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1699/10
1699/50
CGS 15943 | CAS No. 104615-18-1 | Non-selective Adenosine Receptor Antagonists
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Description: Potent adenosine receptor antagonist

Chemical Name: 9-Chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine

Purity: ≥99%

Product Details
Citations (7)
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Biological Activity

CGS 15943 is a potent adenosine receptor antagonist (Ki values are 3.5, 4.2, 16 and 51 nM for human A1, A2A, A2B and A3 receptors respectively). Inhibits the catalytic subunit of the class IB PI3K isoform p110γ (IC50 = 1.1 μM). Blocks HCC and HDAC cell proliferation in vitro via inhibition of the PI3K/Akt pathway; reduces proliferation of ER+ breast cancer cells. Also acts as a BMP-4 mimetic to stimulate osteogenic differentiation. Orally active in vivo.

Technical Data

M.Wt:
285.69
Formula:
C13H8ClN5O
Solubility:
Soluble to 5 mM in DMSO
Purity:
≥99%
Storage:
Store at RT
CAS No:
104615-18-1

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. Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist.
    Ghai et al.
    J.Pharmacol.Exp.Ther., 1987;242:784
  2. Adenosine receptors and their ligands.
    Klot
    Naunyn Schmiedebergs Arch.Pharmacol., 2000;362:382
  3. Biochemical characterization of the triazoloquinazoline CGS 15943, a novel, non-xanthine adenosine antagonist.
    Williams et al.
    J.Pharmacol.Exp.Ther., 1987;241:415

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Citations for CGS 15943

The citations listed below are publications that use Tocris products. Selected citations for CGS 15943 include:

7 Citations: Showing 1 - 7

  1. An Adenosine Receptor for Olfaction in Fish.
    Authors: Wakisaka Et al.
    Curr Biol  2017;27:1437
  2. Activation of P2X7 and P2Y11 purinergic receptors inhibits migration and normalizes tumor-derived endothelial cells via cAMP signaling
    Authors: Avanzato Et al.
    Scientific Reports  2016;6:32602
  3. Purinergic and store-operated Ca(2+) signaling mechanisms in mesenchymal stem cells and their roles in ATP-induced stimulation of cell migration.
    Authors: Peng Et al.
    Stem Cells  2016;34:2102
  4. Application of BRET to monitor ligand binding to GPCRs.
    Authors: Stoddart Et al.
    Nat Methods  2015;12:661
  5. Homeostatic control of synaptic activity by endogenous adenosine is mediated by adenosine kinase.
    Authors: Diógenes Et al.
    Cereb Cortex  2014;24:67
  6. Adenosine release during seizures attenuates GABAA receptor-mediated depolarization.
    Authors: Ilie Et al.
    J Neurosci  2012;32:5321
  7. Constitutive lysosome exocytosis releases ATP and engages P2Y receptors in human monocytes.
    Authors: Sivaramakrishnan Et al.
    J Cell Sci  2012;125:4567

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