CVT-6883

CVT-6883 is an adenosine A2B receptor antagonist (Ki = 22 nM). 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. It also decreases fibrosis in the non-infarct zone, improves ejection fractions, and reduces ventricular tachycardia in a rat model of myocardial infarction.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: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 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.