S85800 |
AZD2098 |
源叶(MedMol) | 99% |
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- 产品描述: AZD2098 is a potent and selective CC-chemokine receptor 4 (CCR4) inhibitor with pIC50s of 7.8, 8.0, 8.0 and 7.6 for human, rat, mouse and dog respectively, used for asthma research
- 靶点: CCR4;CCR
- 体外研究:
AZD2098 potently inhibits chemokine-induced cellular responses, with pIC50 of 7.5 and 6.3 against CCL22-induced Ca2+ influx in hCCR4-expressing CHO cells and CCL17- or CCL22-induced chemotaxis of primary human Th2 cells respectively
- 体内研究:
AZD2098 (73.5-5.0 μg/kg; p.o.; BID; twice a day; 1 hour before and every 12 hours after antigen challenge) exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats, and the changes are first visible at a dose of 0.22 µmol/kg and maximal at 7.5 µmol/kg. Animal Model: Brown-Norway rats Dosage: 73.5 µg/kg, 250.6 µg/kg, 735.2 µg/kg, 1.0 mg/kg, 2.5 mg/kg, 5.0 mg/kg Administration: Oral administration; twice a day; 1 hour before and every 12 hours after antigen challenge Result: Exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats.
- 参考文献:
1. Kindon N, et al. Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists. ACS Med Chem Lett. 2017 Sep 1;8(9):981-986. 2. Asher Mullard. Cancer charity sees success re-prioritizing industry's shelved compounds. Nat Rev Drug Discov. 2014 May;13(5):319-21.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.992 ml 14.962 ml 29.924 ml 5 mM 0.598 ml 2.992 ml 5.985 ml 10 mM 0.299 ml 1.496 ml 2.992 ml 50 mM 0.06 ml 0.299 ml 0.598 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)