MRS2500 (tetraammonium)

MRS2500 tetraammonium is a potent, selective and stable antagonist of the P2Y1 receptor (Ki=0.78 nM for recombinant human P2Y1 receptor) . MRS2500 tetraammonium inhibits the ADP-induced aggregation of human platelets with an IC50 value of 0.95 nM. Antithrombotic activity[1][2][3].

Product Specifications

CAS Number

[630103-23-0]

UNSPSC

12352005

Target

P2Y Receptor

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Purity

99.91

Solubility

H2O : 50 mg/mL (ultrasonic)

Smiles

O=P(O[C@@H]1[C@]2(COP(O[NH4])(O[NH4])=O)C[C@]2([H])[C@@H](N3C=NC4=C(NC)N=C(I)N=C34)C1)(O[NH4])O[NH4]

Molecular Formula

C13H30IN9O8P2

Molecular Weight

629.28

References & Citations

[1]Cattaneo M, et al. Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor. Biochem Pharmacol. 2004;68 (10) :1995-2002.|[2]Wong PC, et al. The P2Y1 receptor antagonist MRS2500 prevents carotid artery thrombosis in cynomolgus monkeys. J Thromb Thrombolysis. 2016;41 (3) :514-521.|[3]Hechler B, et al. MRS2500 [2-iodo-N6-methyl- (N) -methanocarba-2'-deoxyadenosine-3',5'-bisphosphate], a potent, selective, and stable antagonist of the platelet P2Y1 receptor with strong antithrombotic activity in mice. J Pharmacol Exp Ther. 2006;316 (2) :556-563.