AZD1283
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
在结合\GTPγS和残余血小板计数(RPC)试验中的IC50值分别为0.011\0.025和3.2 μM.
P2Y12受体在血小板功能中的主要作用是使其成为研发新型抗血小板治疗的有吸引力的靶点.AZD1283是P2Y12受体的高效选择性可逆抑制剂.
体外实验:苄基AZD1283及其类似物13在高阶残余血小板实验中都具有效应,两种测试的5-氯化联苯都表现出较低(IC50 >22 μM)的效应[1].
体内试验:在修饰的Folts狗模型中,AZD1283及其类似物13能够以剂量依赖的方式诱导血流量提高,并抑制ADP诱导的血小板凝集,抗血栓形成的EC50值分别为3.0和10.0 μg/kg/min.AZD1283和13诱导使流血时间增加3倍的剂量分别为33和100 μg/kg/min [2].
临床试验中:目前尚无临床数据.
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 470.54 |
Cas No. | 919351-41-0 |
Formula | C23H26N4O5S |
Solubility | insoluble in H2O; insoluble in EtOH; ≥18.15 mg/mL in DMSO |
SDF | Download SDF |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
质量控制和MSDS
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