Catalog No.S5358 Synonyms: CVT-3146, Lexiscan
Molecular Weight(MW): 390.35
Regadenoson is a selective A2A adenosine receptor agonist with coronary vasodilating activity.
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|Description||Regadenoson is a selective A2A adenosine receptor agonist with coronary vasodilating activity.|
Regadenoson has a relatively low binding affinity (hA2A Ki=290 nM) for human A2A receptors and greater than 30-fold selectivity versus the A2B and A3AR subtypes and 13-fold over the A1AR. Regadenoson behaves as a weak partial agonist causing cAMP accumulation in PC12 cells but as a full and potent agonist causing coronary vasodilation.
|In vivo||In a dog model, intravenous bolus injection of regadenoson causes a dose-dependent increase in myocardial blood flow and a dose-dependant decrease in coronary vascular resistance. In a rat heart model, regadenoson was shown to have a dose-dependent increase in heart rate and a decrease in mean arterial pressure at the higher doses. Regadenoson also caused more than a 2-fold increase in serum norepinephrine and epinephrine. For clinical data, Regadenoson has a volume of distribution of 11.5 L and 78.7 L (at steady-state), and an estimated clearance of 37.8 L/h. It is renally excreted (58% of total elimination) with a terminal half-life of 33 to 108 min.|
|In vitro||DMSO||56 mg/mL (143.46 mM)|
|Ethanol||56 mg/mL (143.46 mM)|
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