GS 6201

Pricing Availability Delivery Time Qty
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)
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.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

References are publications that support the products' biological activity.

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.

View Related Products by Target

View Related Products by Product Action

View all Adenosine A2B Receptor Antagonists

Keywords: GS 6201, supplier, GS6201, CVT6883, asthma, adenosine, A2B, antagonists, allergy, antiallergics, selective, CVT, 6883, Adenosine, A2B, Receptors, Adenosine, A2B, Receptors, Tocris Bioscience

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


Do you know of a great paper that uses GS 6201 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
Cardiovascular

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

Pathways for GS 6201

Protocols

TODO: Add Protocols