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MRS 2500 tetraammonium salt

Cat. No. 2159

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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 (K_i = 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

M.Wt:

629.29

Formula:

C₁₃H₁₈N₅O₈P₂I.4NH₃

Solubility:

Soluble to 100 mM in water

Purity:

>96 %

Storage:

Store at -20°C

CAS No:

779323-43-2

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

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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