[CAS NO. 313348-27-5]  Regadenoson

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PRODUCTS SPECIFICATIONS [313348-27-5]

Store
Catalog
SLK-S5358
Brand
Selleck
CAS
313348-27-5

DESCRIPTION [313348-27-5]

Overview

MDLMFCD09832544
Molecular Weight390.35
Molecular FormulaC15H18N8O5
SMILESNC1=C2C(N(C=N2)[C@@]3(O[C@H](CO)[C@@H](O)[C@H]3O)[H])=NC(=N1)N4C=C(C(NC)=O)C=N4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.5618 mL12.8090 mL25.6180 mL
5 mM0.5124 mL2.5618 mL5.1236 mL
10 mM0.2562 mL1.2809 mL2.5618 mL
50 mM0.0512 mL0.2562 mL0.5124 mL

Description

Regadenoson (CVT-3146, Lexiscan) is a selective 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.

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.


Synonyms

Adenosine, 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]-
2-[4-[(Methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine
CVT 3146
Regadenoson
Lexiscan
NQZ-021
CV 3146
Rapiscan