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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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 470.54. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.13 mL||10.63 mL||21.25 mL|
|5 mM||0.43 mL||2.13 mL||4.25 mL|
|10 mM||0.21 mL||1.06 mL||2.13 mL|
|50 mM||0.04 mL||0.21 mL||0.43 mL|
References are publications that support the biological activity of the product.
Bach et al (2013) 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. J.Med.Chem. 56 7015 PMID: 23899349
Zhang et al (2014) Agonist-bound structure of the human P2Y12 receptor. Nature 509 119 PMID: 24784220
Zhang et al (2014) Structure of the human P2Y12 receptor in complex with an antithrombotic drug. Nature 509 115 PMID: 24670650
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Keywords: AZD 1283, AZD 1283 supplier, AZD1283, High, affinity, p2y12, purine, receptors, antagonists, purinoceptors, purinergic, antagonises, inhibitors, inhibits, Purinergic, P2Y, Receptors, 6085, Tocris Bioscience
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