Chemical Name: Ethyl 5-cyano-2-methyl-6-[4-[[[(phenylmethyl)sulfonyl]amino]carbonyl]-1-piperidinyl]-3-pyridinecarboxylate
Biological ActivityAZD 1283 is a potent and high affinity P2Y12 antagonist (IC50 = 11 nM in radioligand competition binding assay, and 25 nM in a GTPγS binding assay). Causes a dose-dependent increase in blood flow and inhibits ADP-induced platelet aggregation in vivo. Antithrombotic.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283.
Bach et al.
Agonist-bound structure of the human P2Y12 receptor.
Zhang et al.
Structure of the human P2Y12 receptor in complex with an antithrombotic drug.
Zhang et al.
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