Regadenoson

Catalog No.S5358 Synonyms: CVT-3146, Lexiscan

Regadenoson Chemical Structure

Molecular Weight(MW): 390.35

Regadenoson is a selective A2A adenosine receptor agonist with coronary vasodilating activity.

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Biological Activity

Description Regadenoson is a selective A2A adenosine receptor agonist with coronary vasodilating activity.
Targets
A2AR [1]
()
290 nM(Ki)
In vitro

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[1].

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[2].

Protocol

Solubility (25°C)

In vitro DMSO 56 mg/mL (143.46 mM)
Ethanol 56 mg/mL (143.46 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 390.35
Formula

C15H18N8O5

CAS No. 313348-27-5
Storage powder
in solvent
Synonyms CVT-3146, Lexiscan

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