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Submit ReviewAZD 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.
AZD 1283 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 470.54 |
公式 | C23H26N4O5S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 919351-41-0 |
PubChem ID | 23649325 |
InChI Key | NEMHKCNXXRQYRF-UHFFFAOYSA-N |
Smiles | CCOC(C1=CC(C#N)=C(N2CCC(C(NS(=O)(CC3=CC=CC=C3)=O)=O)CC2)N=C1C)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 47.05 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for AZD 1283, please let us know.
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