For research use only. Not for therapeutic Use.
GS-6201 (CAT: I011872) is a potent and selective adenosine A₂B receptor antagonist with high affinity for the human receptor (Ki = 22 nM). It demonstrates cardioprotective activity by reducing caspase-1 activity and attenuating cardiac remodeling after acute myocardial infarction in mice. Repeated intraperitoneal administration (4 mg/kg, twice daily) significantly lowers pro-inflammatory mediators including IL-6, TNF-α, E-selectin, ICAM-1, and VCAM, while preventing ventricular enlargement and dysfunction for up to 28 days. In respiratory models, GS-6201 suppresses airway hyperreactivity induced by NECA, AMP, or allergens. Pharmacokinetic studies show good oral bioavailability (Cmax = 1110 ng/mL; t½ = 4.25 h).
| CAS Number | 752222-83-6 |
| Synonyms | 3-ethyl-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]-7H-purine-2,6-dione |
| Molecular Formula | C21H21F3N6O2 |
| Purity | ≥95% |
| IUPAC Name | 3-ethyl-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]-7H-purine-2,6-dione |
| InChI | 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) |
| InChIKey | KOYXXLLNCXWUNF-UHFFFAOYSA-N |
| SMILES | CCCN1C(=O)C2=C(N=C(N2)C3=CN(N=C3)CC4=CC(=CC=C4)C(F)(F)F)N(C1=O)CC |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
