1. GPCR/G Protein
    Neuronal Signaling
    Membrane Transporter/Ion Channel
  2. Adenosine Receptor
    Calcium Channel
  3. MRS 1523

MRS 1523 

Cat. No.: HY-121119
Handling Instructions

MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons.

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MRS 1523 Chemical Structure

MRS 1523 Chemical Structure

CAS No. : 212329-37-8

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Description

MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons[1][2].

IC50 & Target

Ki: 18.9 nM (Human A3 receptor), 113 nM (Rat A3 receptor), 15.6 µM (A1 receptor) and 2.05 µM (A2A receptor)[1]

In Vitro

MRS 1523 (0.1-1 μM) treatment significantly antagonizes cell numbers to 40.7% and 57.4% of the control values, respectively, 30 min before the addition of cordycepin (60 μM). MRS1523 (1 μM) alone has any effect on tumor cell growth[3].
A partial blockade of the adenosine-5'-N-ethylcarboxamide (NECA)-induced migration is observed when human endothelial progenitor cells (hEPC) are co-incubated with MRS 1523 (1 nM). Furthermore, in 3-days hEPC, the treatment with MRS 1523 100 nM inhibits the NECA-induced migration by 70%. NECA-induced migration is blocked in dose-response fashion by MRS 1523 with calculated Ki of 147 nM[4].

Cell Viability Assay[3]

Cell Line: B16-BL6 cells
Concentration: 0.1 µM, 1 µM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Antagonized the growth suppression induced by cordycepin.
In Vivo

The expression and functional effects of A3 adenosine receptor (A3AR) on the excitability of small- to medium-sized, capsaicin-sensitive, dorsal root ganglion (DRG) neurons isolated from 3- to 4-week-old rats are investigated. The endogenous agonist adenosine reduces N-type Ca currents, and its effect is inhibited by 56% in the presence of A3AR antagonist MRS 1523. Current-clamp recordings demonstrated that neuronal firing of rat DRG neurons was also significantly reduced by A3AR activation in a MRS 1523-sensitive but PD173212-insensitive manner[2].

Molecular Weight

399.55

Formula

C₂₃H₂₉NO₃S

CAS No.

212329-37-8

SMILES

O=C(OCCC)C1=C(C(C(SCC)=O)=C(N=C1C2=CC=CC=C2)CC)CCC

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

MRS 1523MRS1523MRS-1523Adenosine ReceptorCalcium ChannelP1 receptorCa2+ channelsCa channelsA3-receptormigrationantihyperalgesicN-typeCa-channelneuronsInhibitorinhibitorinhibit

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MRS 1523
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