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Submit ReviewGS 6201
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)
Biological Activity for GS 6201
GS 6201 is a 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.
Compound Libraries for GS 6201
GS 6201 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GS 6201
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GS 6201
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 2.23 | 5 |
Preparing Stock Solutions for GS 6201
The following data is based on the product molecular weight 446.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.05 mM | 44.8 mL | 224 mL | 448 mL |
| 0.25 mM | 8.96 mL | 44.8 mL | 89.6 mL |
| 0.5 mM | 4.48 mL | 22.4 mL | 44.8 mL |
| 2.5 mM | 0.9 mL | 4.48 mL | 8.96 mL |
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Product Datasheets for GS 6201
References for GS 6201
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
If you know of a relevant reference for GS 6201, please let us know.
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Keywords: GS 6201, GS 6201 supplier, GS6201, CVT6883, asthma, adenosine, A2B, antagonists, allergy, antiallergics, selective, CVT, 6883, Adenosine, Receptors, 4727, Tocris Bioscience
3 Citations for GS 6201
Citations are publications that use Tocris products. Selected citations for GS 6201 include:
Qun et al (2019) The Role of Adenosine A2b Receptor in Mediating the Cardioprotection of Electroacupuncture Pretreatment via Influencing Ca2+ Key Regulators. Evid Based Complement Alternat Med 2019 6721286 PMID: 31885657
Mertens et al (2018) Switching-Off Adora2b in Vascular Smooth Muscle Cells Halts the Development of Pulmonary Hypertension. Front Physiol 9 555 PMID: 29910735
Perez-Aso et al (2015) A novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Arthritis Res Ther 17 249 PMID: 26370839
Do you know of a great paper that uses GS 6201 from Tocris? Please let us know.
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