切换导航

AZD1283

现货
Catalog No.
B4634
P2Y12拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,650.00
现货
5mg
¥ 1,500.00
现货
10mg
¥ 2,600.00
现货
50mg
¥ 6,500.00
现货
100mg
¥ 8,500.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

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, Björkman JA, Österlund 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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt470.54
Cas No.919351-41-0
FormulaC23H26N4O5S
Solubility≥18.15mg/mL in DMSO
SDFDownload SDF
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

动物实验 [1]:

动物模型

修饰的Folts犬模型

给药剂量

0.1 ~ 33 μg/(kg × min);每隔30分钟给药,一共给药5次

实验结果

AZD1283呈剂量依赖性地增加血流量并抑制ADP诱导的血小板聚集,其抗血栓形成的ED50值为3 μg/(kg × min)。使出血时间增加至3.5倍以上需要高于33 μg/(kg × min)的剂量。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Bach P, Antonsson T, Bylund R, Bjrkman 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.

质量控制