| 产品描述： | CXCR4 选择性抑制剂 | 激动剂 | 拮抗剂;CXCR4 Selective Inhibitors | Agonists | Antagonists;;InformationLIT-927 is a novel neutraligand ofCXCL12with Ki value of 267 nM for inhibition of Texas red-labeled CXCL12 (CXCL12-TR) binding. It shows high selectivity toward CXCL12 vs other chemokines also involved in asthma.TargetsCXCR4 ; CXCL12 ; 267 nM(Ki)In vitroLIT-927 is able to bind selectively CXCL12 and to inhibit CXCL12-CXCR4 interaction.In vivoIn a murine model of hypereosinophilia, LIT-927 shows a large and statistically reliable inhibition of eosinophil recruitment. It inhibits allergic eosinophilic airway inflammation in mice when administered orally or locally. |
| 体内研究： |
LIT-927 (compound 57) reduces eosinophil recruitment in a murine model of allergic airway hypereosinophilia, LIT-927 is the only one to display inhibitory activity following oral administration. Combined with a high binding selectivity for CXCL12 over other chemokines, LIT-927 represents a powerful pharmacological tool to investigate CXCL12 physiology in vivo and to explore the activity of chemokine neutralization in inflammatory and related diseases. |
| 参考文献： |
1. Regenass P, et al. Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a Murine Model of Allergic Airway Hypereosinophilia. J Med Chem. 2018 Sep 13;61(17):7671-7686. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.042 ml |
15.209 ml |
30.418 ml |
| 5 mM |
0.608 ml |
3.042 ml |
6.084 ml |
| 10 mM |
0.304 ml |
1.521 ml |
3.042 ml |
| 50 mM |
0.061 ml |
0.304 ml |
0.608 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京