GS-6201

GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM) [1]. GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse[2]. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice[3].

Product Specifications

CAS Number

[752222-83-6]

Product Name Alternative

CVT-6883

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Adenosine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/gs-6201.html

Purity

99.72

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(N1CCC)N(CC)C2=C(N=C(C3=CN(CC4=CC=CC(C(F)(F)F)=C4)N=C3)N2)C1=O

Molecular Formula

C21H21F3N6O2

Molecular Weight

446.43

Precautions

H302, H315, H319

References & Citations

[1]Elzein E, et al. Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. J Med Chem. 2008 Apr 10;51 (7) :2267-78.|[2]Toldo S, et al. GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J Pharmacol Exp Ther. 2012 Dec;343 (3) :587-95.|[3]Mustafa SJ, et al. Effect of a specific and selective A (2B) 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. 2007 Mar;320 (3) :1246-51.