Cat. No. 2158
Chemical Name: (1R*,2S*)-4-[2-Chloro-6-(methylamin
Biological ActivitySelective, 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).
Licensing InformationSold under license from the NIH, US Patent 10/169975
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 / Product Datasheet / Safety Data Sheet
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.
Boyer et al (2002) 2-Chloro N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate is a selective high affinity P2Y1 receptor antagonist. Br.J.Pharmacol. 135 2004. PMID: 11959804.
Nandanan et al (2000) Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y1 receptor ligands. J.Med.Chem. 43 829. PMID: 10715151.
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Citations are publications that use Tocris products. Selected citations for MRS 2279 include:
Kuboyama et al (2011) Astrocytic P2Y(1) receptor is involved in the regulation of cytokine/chemokine transcription and cerebral damage in a rat model of cerebral ischemia. Cell Death Dis 31 1930. PMID: 21487414.
Ohtomo et al (2011) Increase of intracellular Ca2+ by purinergic receptors in cultured rat lacrimal gland myoepithelial cells. Invest Ophthalmol Vis Sci 52 9503. PMID: 22039237.
Harper and Poole (2010) Protein kinase Ctheta negatively regulates store-independent Ca2+ entry and phosphatidylserine exposure downstream of glycoprotein VI in platelets. J Biol Chem 285 19865. PMID: 20388711.
Do you know of a great paper that uses MRS 2279 from Tocris? If so please let us know.
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Keywords: MRS 2279, supplier, Selective, high, affinity, P2Y1, antagonists, Receptors, Purinergic, purinoceptors, MRS2279, Tocris Bioscience, Purinergic (P2Y) Receptor Antagonist products
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