MRS542

MRS542 is a nucleoside A3 AR antagonist with a pKi of 8.74. MRS542 also acts as a partial agonist (pEC50 = 7.76) in promoting β-arrestin translocation. MRS542 can be converted into an agonist by LUF6000 (HY-13236) . MRS542 can be used for cardiovascular disease research[1][2].

Product Specifications

CAS Number

[163152-31-6]

UNSPSC

12352005

Target

Adenosine Receptor; Arrestin

Related Pathways

GPCR/G Protein

Field of Research

Cardiovascular Disease

Smiles

N(CC1=CC(I)=CC=C1)C2=C3C(N(C=N3)[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)=NC(Cl)=N2

Molecular Formula

C17H17ClIN5O4

Molecular Weight

517.71

References & Citations

[1]Gao ZG, et al. Translocation of arrestin induced by human A (3) adenosine receptor ligands in an engineered cell line: comparison with G protein-dependent pathways. Pharmacol Res. 2008 Apr;57 (4) :303-11.|[2]Gao ZG, et al. Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000. BMC Pharmacol. 2008 Dec 12;8:20.