MRS 2500 tetraammonium salt
Names
[ CAS No. ]:
630103-23-0
[ Name ]:
MRS 2500 tetraammonium salt
[Synonym ]:
[(1R,2S,4S,5S)-4-[2-Iodo-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hex-1-yl]methyl dihydrogen phosphate tetraammoniate
Bicyclo[3.1.0]hexane-1-methanol, 4-[2-iodo-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)-, dihydrogen phosphate (ester), tetraammonium salt, (1R,2S,4S,5S)-
Biological Activity
[Description]:
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].
[Related Catalog]:
[In Vitro]
MRS2500 tetraammonium inhibits platelet aggregation to 10 μM ADP with an IC50 of 0.95 nM in human washed platelets. MRS2500 tetraammonium inhibits platelet aggregation to 10μM ADP with an IC50 of 0.49 μM in human PRP[4].
[In Vivo]
MRS2500 (2 mg/kg; i.v.) decreases acute systemic thromboembolism through selective inhibition of the P2Y1 receptor[3]. MRS2500 exhibited strong antithrombotic efficacy in the prevention of arterial thrombosis in the monkey ECAT model[4].. Animal Model: 20-25 g WT Male mice (acute vascular occlusion model)[3] Dosage: 2 mg/kg Administration: Intravenous Result: Reduced platelet consumption.
[References]
[1]. 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.
[2]. Cattaneo M, et al. Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor. Biochem Pharmacol. 2004;68(10):1995-2002.
[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.
[4]. Wong PC, et al. The P2Y1 receptor antagonist MRS2500 prevents carotid artery thrombosis in cynomolgus monkeys. J Thromb Thrombolysis. 2016;41(3):514-521.
Chemical & Physical Properties
[ Molecular Formula ]:
C13H30IN9O8P2
[ Molecular Weight ]:
629.285
[ Exact Mass ]:
629.073730