| 產(chǎn)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 |
| 靶點(diǎn)： |
CCR4;CCR |
| 體外研究： |
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 |
| 體內(nèi)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. |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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 |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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