MRS 2279
Chemical Name: (1R*,2S*)-4-[2-Chloro-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hexane-1-methanol dihydrogen phosphate ester diammonium salt
Purity: ≥98%
Biological Activity
MRS 2279 is a selective, high affinity competitive antagonist of the P2Y1 receptor (Ki = 2.5 nM; IC50 = 51.6 nM). Fails to block nucleotide signaling at most other P2Y receptors (P2Y2, P2Y4, P2Y6, P2Y11 and P2Y12) and potently inhibits ADP-induced aggregation of human blood platelets in vitro (pKB = 8.05).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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SDF-1alpha is a novel autocrine activator of platelets operating through its receptor CXCR4.
Walsh T, Harper M, Poole A
Cell Signal, 2015;27(1):37-46. -
RhoG protein regulates platelet granule secretion and thrombus formation in mice.
Goggs R, Harper M, Pope R, Savage J, Williams C, Mundell S, Heesom K, Bass M, Mellor H, Poole A
J Biol Chem, 2013;288(47):34217-29. -
?-Nicotinamide Adenine Dinucleotide (?-NAD) Inhibits ATP-Dependent IL-1? Release from Human Monocytic Cells
SD Hiller, S Heldmann, K Richter, I Jurastow, M Küllmar, A Hecker, S Wilker, G Fuchs-Moll, I Manzini, G Schmalzing, W Kummer, W Padberg, JM McIntosh, J Damm, A Zakrzewicz, V Grau
Int J Mol Sci, 2018;19(4):. -
Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y1 receptor ligands.
Nandanan et al.
J.Med.Chem., 2000;43:829 -
2-Chloro N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate is a selective high affinity P2Y1 receptor antagonist.
Boyer et al.
Br.J.Pharmacol., 2002;135:2004 -
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.
Kim et al.
J.Med.Chem, 2003;46:4974
Product Datasheets
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Citations for MRS 2279
The citations listed below are publications that use Tocris products. Selected citations for MRS 2279 include:
5 Citations: Showing 1 - 5
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Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
Authors: Dosch Et al.
Elife 2019;8
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P2X7 receptor-pannexin 1 interaction mediates extracellular alpha-synuclein-induced ATP release in neuroblastoma SH-SY5Y cells.
Authors: Wilkaniec Et al.
Purinergic Signal 2017;13:347
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Increase of intracellular Ca2+ by purinergic receptors in cultured rat lacrimal gland myoepithelial cells.
Authors: Ohtomo Et al.
Invest Ophthalmol Vis Sci 2011;52:9503
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Astrocytic P2Y(1) receptor is involved in the regulation of cytokine/chemokine transcription and cerebral damage in a rat model of cerebral ischemia.
Authors: Kuboyama Et al.
Cell Death Dis 2011;31:1930
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Protein kinase Ctheta negatively regulates store-independent Ca2+ entry and phosphatidylserine exposure downstream of glycoprotein VI in platelets.
Authors: Harper and Poole
J Biol Chem 2010;285:19865
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