GS 6201

Cat. No. 4727

GS 6201 C21H21F3N6O2 [752222-83-6]

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Alternative Name: 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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Toldo et al (2012) GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J.Pharmacol.Exp.Ther. 343 587. PMID: 22923737.

Elzein et al (2008) Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. J.Med.Chem. 51 2267. PMID: 18321039.

Mustafa et al (2007) 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. J.Pharmacol.Exp.Ther. 320 1246. PMID: 17159162.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for GS 6201 include:

Perez-Aso et al (2015) Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Arthritis Res Ther 17 249. PMID: 26370839.

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Keywords: GS 6201, supplier, GS6201, CVT6883, asthma, adenosine, A2B, antagonists, allergy, antiallergics, selective, Tocris Bioscience, Adenosine A2B Receptor Antagonist products

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