GS 6201

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Cat.No. 4727 - GS 6201 | C21H21F3N6O2 | CAS No. 752222-83-6
Description: Selective A2B antagonist
Alternative 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
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

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
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 752222-83-6
PubChem ID 11270783
InChI Key KOYXXLLNCXWUNF-UHFFFAOYSA-N
Smiles O=C(N(CC)C2=C1NC(C3=CN(CC4=CC=CC(C(F)(F)F)=C4)N=C3)=N2)N(CCC)C1=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 2.23 5

Preparing Stock Solutions

The following data is based on the product molecular weight 446.43. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.24 mL 11.2 mL 22.4 mL
5 mM 0.45 mL 2.24 mL 4.48 mL
10 mM 0.22 mL 1.12 mL 2.24 mL
50 mM 0.04 mL 0.22 mL 0.45 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

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

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

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


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1 Citation for GS 6201

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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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

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