MRS 1523

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].

Product Specifications

CAS Number

[212329-37-8]

UNSPSC

12352005

Hazard Statement

H225, H319

Target

Adenosine Receptor; Calcium Channel

Type

Reference compound

Related Pathways

GPCR/G Protein; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/mrs-1523.html

Purity

99.97

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C23H29NO3S

Molecular Weight

399.55

Precautions

H225, H319

References & Citations

[1]Li AH, et al. Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.J Med Chem. 1998 Aug 13;41 (17) :3186-201.|[2]Coppi E, et al. Adenosine A3 receptor activation inhibits pronociceptive N-type Ca2+ currents and cell excitability in dorsal root ganglion neurons.Pain. 2019 May;160 (5) :1103-1118.|[3]Fernandez P, et al. Adenosine A₂A and A₃ receptors are involved in the human endothelial progenitor cells migration. J Cardiovasc Pharmacol. 2012 May;59 (5) :397-404.|[4]Yoshikawa N, et al. Cordycepin (3'-deoxyadenosine) inhibits the growth of B16-BL6 mouse melanoma cells through the stimulation of adenosine A3 receptor followed by glycogen synthase kinase-3beta activation and cyclin D1 suppression. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jun;377 (4-6) :591-5.