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AZD1283
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AZD1283图片
CAS NO:919351-41-0
规格:98%
分子量:470.54
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Potent P2Y12 antagonist
CAS:919351-41-0
分子式:C23H26N4O5S
分子量:470.54
纯度:98%
存储:Store at -20°C

Background:

IC50: 0.011, 0.025 and 3.2 μM for binding, GTPγS and residual platelet count (RPC), respectively


The central role of the P2Y12 receptor in platelet function makes it an attractive target for the development of novel antiplatelet therapies. AZD1283 is found to be a potent, selective and reversible antagonist of the P2Y12 receptor.


In vitro: It was observed that the benzylic AZD1283 and its analogue 13 were both potent in the higher order residual platelet count assay in which the two tested 5-chlorothienyls showed low (IC50 >22 μM) potency [1].


In vivo: In a modified Folts model in dog, both AZD1283 and its analogue 13 could dose-dependently induce increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10.0 μg/kg/min, respectively. The dose that induced a larger than 3-fold increase in bleeding time were 33 and 100 μg/kg/min for AZD1283 and 13, respectively [2].


Clinical trials: Currenlty there is no clinical data available.


Reference:
[1] Bach P, Antonsson T, Bylund R, Bj?rkman JA, ?sterlund K, Giordanetto F, van Giezen JJ, Andersen SM, Zachrisson H, Zetterberg F.   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. 2013;56(17):7015-24.