An adenosine A2B receptor antagonist
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CVT-6883

Item No. 33333

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-ethyl-3,9-dihydro-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-4-yl]-1H-purine-2,6-dione
CAS Number
752222-83-6
Synonyms
  • GS-6201
Molecular Formula
C21H21F3N6O2
Formula Weight
446.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
236, 304 nm
SMILES
O=C1C2=C(N(CC)C(N1CCC)=O)N=C(C3=CN(CC4=CC=CC(C(F)(F)F)=C4)N=C3)N2O=C1C2=C(N(CC)C(N1CCC)=O)N=C(C3=CN(CC4=CC=CC(C(F)(F)F)=C4)N=C3)N2
InChi Code
InChI=1S/C21H21F3N6O2/c1-3-8-30-19(31)16-18(29(4-2)20(30)32)27-17(26-16)14-10-25-28(12-14)11-13-6-5-7-15(9-13)21(22,23)24/h5-7,9-10,12H,3-4,8,11H2,1-2H3,(H,26,27)
InChi Key
KOYXXLLNCXWUNF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    CVT-6883 is an adenosine A2B receptor antagonist (Ki = 22 nM).1 It is selective for adenosine A2B over adenosine A1, A2A, and A3 receptors (Kis = 1,940, 3,280, and 1,070 nM, respectively), as well as a panel of 84 receptors, ion channels, transporters, and enzymes at 10 µM. CVT-6883 (6 mg/kg) decreases allergen challenge-induced bronchoalveolar lavage fluid (BALF) eosinophil and lymphocyte infiltration and airway reactivity in a mouse model of allergic asthma.2 It also decreases fibrosis in the non-infarct zone, improves ejection fractions, and reduces ventricular tachycardia in a rat model of myocardial infarction.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Elzein, E., Kalla, R.V., Li, X., et al. Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. J. Med. Chem. 51(7), 2267-2278 (2008).

    2. Mustafa, S.J., Nadeem, A., Fan, M., et al. 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(3), 1246-1251 (2007).

    3. Zhang, H., Zhong, H., Everett, T.H., 4th, et al. Blockade of A2B adenosine receptor reduces left ventricular dysfunction and ventricular arrhythmias 1 week after myocardial infarction in the rat model. Heart Rhythm 11(1), 101-109 (2014).