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Regadenoson

Name: Regadenoson
Brand: Selleck Chemicals
SKU: S5358
Rating: 5 (1 reviews)

Synonyms: CVT-3146, Lexiscan

Catalog No.S5358 Purity:99.83%

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

Regadenoson Chemical Structure

CAS No. 313348-27-5

Purity & Quality Control

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

99.83

Regadenoson Related Products

Related Targets	Adenosine A1 receptor	Click to Expand
Related Products	Reversine CGS 21680 HCl ZM241385 SCH58261 A2AR antagonist 1 Ciforadenant (CPI-444) Imaradenant (AZD4635)	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ GPCR Compound Library	Click to Expand

Biological Activity

Description

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

Targets

A2AR ^[1]

290 nM(Ki)

In vitro
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 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].

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

Chemical Information & Solubility

Molecular Weight	390.35	Formula	C₁₅H₁₈N₈O₅
CAS No.	313348-27-5	SDF	--
Smiles	CNC(=O)C1=CN(N=C1)C2=NC(=C3C(=N2)N(C=N3)C4C(C(C(O4)CO)O)O)N
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 78 mg/mL ( (199.82 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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Molarity Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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