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Category:
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7TM Receptors P2Y ReceptorsAntagonists
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Cat.No.
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Product Name
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2158 |
MRS 2279
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Price and Availability
Click here for full price details of
MRS 2279
Other Information:
Sold under
licence from the NIH, US Patent 10/169975
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Chemical Name:
(1R,2S,4S,5S)-4-[2-Chloro-6-(methylamino)-9H-purin-9-yl
]-2-(phosphonooxy)bicyclo[3.1.0]hexane-1-methanol
dihydrogen phosphate ester diammonium salt |
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Biological Activity:
Selective, high affinity competitive antagonist of the P2Y1
receptor (Ki = 2.5 nM; IC50 = 51.6 nM). Fails to block
nucleotide signalling 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).
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
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. 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. 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.
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Keywords: MRS 2279, P2Y Receptors, Selective, High Affinity P2Y1 Antagonist, MRS2279, Tocris Bioscience
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| “Our laboratory loves dealing with Tocris and consider many of the compounds you sell to be far better quality than the compounds that we have received from other companies. Once again, thank you very much..” Researcher, Albany Medical College, USA |
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