S87274 |
AZD1283 |
| 源叶(MedMol) | 98% |
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- 产品描述： AZD1283 is a potent P2Y12 receptor antagonist with a binding IC50 of 11 nM and a GTPγS IC50 of 25 nM. AZD1283 has excellent antiplatelet aggregation potency. AZD1283 can be used to research thromboembolic disorders
- 靶点： P2Y12 Receptor:11 nM (IC50)
- 体外研究： AZD1283 exhibits excellent antiplatelet aggregation potency with an IC50 value of 3.6 μM. AZD1283 has highly inhibitory activity against CYP450 with IC50 values of 6.62 μM, 0.399 μM and 4.28 μM and 3.64 μM for CYP2C9, CYP2C19, CYP3A4 (Midazolam as the substrate) and CYP3A4 (Testosterone as the substrate), respectively. AZD1283 induces increases in blood flow and inhibition of ADP-induced platelet aggregation with an antithrombotic EC50 value of 3 μg/(kg×min)
- 体内研究： AZD1283 exhibits poor liver microsomal stability in rat (T1/2 = 6.08 min), but better in dog microsomes (T1/2 = 201 min) and human microsomes (T1/2 = 65.0 min). Animal Model: Sprague-Dawley rats Dosage: 5 mg/kg Administration: p.o.; single dosage Result: Exhibited a Cmax of 25.9 ± 11 ng/mL, a T1/2 of 1.68 ± 0.37 h and a Tmax of 0.25 h.
- 参考文献：
1. Kong D, et al. Optimization of P2Y12 Antagonist Ethyl 6-(4-((Benzylsulfonyl)carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate (AZD1283) Led to the Discovery of an Oral Antiplatelet Agent with Improved Druglike Properties. J Med Chem. 2019 Mar 28;62(6):3088-3106. 2. Bach P, et al. 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 Sep 12;56(17):7015-24.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.125 ml 10.626 ml 21.252 ml 5 mM 0.425 ml 2.125 ml 4.25 ml 10 mM 0.213 ml 1.063 ml 2.125 ml 50 mM 0.043 ml 0.213 ml 0.425 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
