Home GPCR & G Protein Adenosine Receptor agonist Regadenoson

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Regadenoson Adenosine Receptor agonist

Cat.No.S5358

Regadenoson (CVT-3146, Lexiscan) is a selective A2A adenosine receptor agonist with coronary vasodilating activity.
Regadenoson Adenosine Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 390.35

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Quality Control

Batch: S535801 DMSO]78 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.83%
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99.83

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (199.82 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 390.35 Formula

C15H18N8O5

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 313348-27-5 -- Storage of Stock Solutions

Synonyms CVT-3146, Lexiscan Smiles CNC(=O)C1=CN(N=C1)C2=NC(=C3C(=N2)N(C=N3)C4C(C(C(O4)CO)O)O)N

Mechanism of Action

Targets/IC50/Ki
A2AR
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. This compound 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, this compound was shown to have a dose-dependent increase in heart rate and a decrease in mean arterial pressure at the higher doses. It also caused more than a 2-fold increase in serum norepinephrine and epinephrine. For clinical data, this chemical 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04604782 Recruiting
Myocardial Ischemia|Coronary Artery Disease
GE Healthcare|Covance
 May 20 2021 Phase 1|Phase 2
NCT03917199 Completed
Myocardial Perfusion Imaging|Computed Tomography|Coronary Artery Disease
National Institute of Cardiology Warsaw Poland|National Science Centre Poland
 November 2016 --
NCT01919450 Completed
Myocardial Blood Flow Reserve
Timothy M. Bateman MD|Cardiovascular Imaging Technologies
 July 2013 Phase 4

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