MRS 2500 tetraammonium salt

Cat. No. 2159

MRS 2500 tetraammonium salt C13H18N5O8P2I.4NH3 [630103-23-0]

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Chemical Name: (1R*,2S*)-4-[2-Iodo-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hexane-1-methanol dihydrogen phosphate ester tetraammonium salt

Biological Activity

Highly potent and selective antagonist of the platelet P2Y1 receptor (Ki = 0.78 nM). Inhibits ADP-induced aggregation of human platelets with an IC50 value of 0.95 nM. Inhibits the upregulation of NTPDase1 by ATPγS. Prevents thrombus formation in vivo.

Licensing Information

Sold under license from the NIH, US Patent 10/169975

Technical Data

Soluble to 100 mM in water
>96 %
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Kim et al (2003) 2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists. J.Med.Chem 46 4974. PMID: 14584948.

Cattaneo et al (2004) Antiaggregatory activity in human platelets of potent antagonists of the P2Y1 receptor. Biochem.Pharmacol. 68 1995. PMID: 15476670.

Hechler et al (2006) 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. 316 556. PMID: 16236815.

Lu et al (2007) Stimulation of the P2Y1 receptor up-regulates nucleoside-triphosphate diphosphohydrolase-1 in human retinal pigment epithelial cells. J.Pharmacol.Exp.Ther. 323 157. PMID: 17626796.

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Keywords: MRS 2500 tetraammonium salt, supplier, potent, selective, P2Y1, antagonists, Receptors, Purinergic, purinoceptors, MRS2500, prevents, thrombus, formation

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