630103-23-0

630103-23-0 structure

Name: MRS 2500 tetraammonium salt
Chemical Name: [(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
CAS Number: 630103-23-0
Molecular Formula: C₁₃H₃₀IN₉O₈P₂
Molecular Weight: 629.285
Catalog: Signaling Pathways GPCR/G Protein P2Y Receptor
Create Date: 2018-06-05 08:15:53
Modify Date: 2024-01-05 12:53:10
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].

Name	[(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
Synonyms	[(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)-

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	Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> P2Y Receptor
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.

Molecular Formula	C₁₃H₃₀IN₉O₈P₂
Molecular Weight	629.285
Exact Mass	629.073730

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