Catalog Number: 4727
Alternate Names: CVT 6883
Chemical Name: 3-Ethyl-3,9-dihydro-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-4-yl]-1H-purine-2,6-dione
Biological Activity
Selective antagonist of adenosine A2B receptors (Ki values are 22, 1070, 1940 and 3280 nM for human A2B, A3, A1 and A2A receptors respectively). Attenuates allergen-, NECA- and AMP-induced airway reactivity in an allergic mouse model of asthma. Also shown to attenuate the inflammatory response during acute myocardial infarction in mice; reduces caspase-1 activity in the heart.
Technical Data
  • M.Wt:
    446.43
  • Formula:
    C21H21F3N6O2
  • Solubility:
    Soluble to 5 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    752222-83-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases.
    Elzein et al.
    J.Med.Chem., 2008;51:2267
  2. GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse.
    Toldo et al.
    J.Pharmacol.Exp.Ther., 2012;343:587
  3. Effect of a specific and selective A2B adenosine receptor antagonist on adenosine agonist AMP and allergen-induced airway responsiveness and cellular influx in a mouse model of asthma.
    Mustafa et al.
    J.Pharmacol.Exp.Ther., 2007;320:1246
Citations:

The citations listed below are publications that use Tocris products. Selected citations for GS 6201 include:

1 Citations: Showing 1 - 1

  1. Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors.
    Authors: Perez-Aso Et al.
    Arthritis Res Ther 2015;17:249

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