Network Version
Product Name: | Capadenoson | |
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CAS No.: | 544417-40-5 | |
Cat. No.: | HY-14917 | |
MWt: | 520.03 | |
Formula: | C25H18ClN5O2S2 | |
Purity : | >98% | |
Solubility: | DMSO : ≥ 50 mg/mL (96.15 mM); H2O : < 0.1 mg/mL (insoluble) | |
Mechanisms: | Target: Cardiovascular Disease | |
Biological Activity: | ||
Capadenoson is a selective agonist of adenosine-A1 receptor. IC50 & Target: Adenosine A1 receptor[1] In Vitro: To further elucidate the pharmacological properties of Capadenson, GTP shift assays are performed with the standard full A1-agonist CCPA and the A1-antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX). CCPA shows a Ki value of 4.2 nM in the binding assay on rat cortical brain membranes. In the presence of 1 mM GTP this Ki value shifts to a value of 64 nM. Therefore the GTP shift for CCPA is 15. DPCPX shows a GTP shift of 1 with virtually identical Ki values in the absence and presence of GTP. Capadenson shows a Ki value of 24 nM in the binding assay. In the presence of 1 mM GTP this Ki value shifts to a value of 116 nM resulting in a GTP shift of 5 for Capadenoson[1]. In Vivo: In the in vivo experiments, Wistar rats and SHR are pre-treated with Capadenoson at a concentration of 0.15 mg/kg for 5 days. On day 5, a stress test (physical restraint) is performed for 2 hours. The plasma concentration of Capadenoson measured 3 hours after drug intake remains constant in the 5 days prior to the restraint stress test and averaged 7.63 µg/L on day 4 and 5, respectively[1]. |
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