| 产品描述： | Sibofimloc (Antibiotic-202) is a first-in-class, gut-restricted, orally active FimH adhesion inhibitor extracted from patent WO2014100158A1, Compound Example 202. Sibofimloc has anti-bacterial infective activity. Sibofimloc is developed for inflammatory bowel disease (IBD) |
| 靶点： |
FimH adhesion |
| 体外研究： |
FimH is a TLR4 receptor, expressed on E. coli and other Enterobacteriaceae in host with CD. The inhibition of FimH adhesion, and consequently intracellular replication of adherent-invasive E. coli in epithelial cells, may prevent establishment of a sub-mucosal infection leading to mucosal inflammation and epithelial barrier disruption |
| 参考文献： |
1. Ramtohul, Yeeman K, et al. Preparation of mannose derivatives via coupling and click cycloaddition reactions for treating bacterial infections. From PCT Int. Appl. (2014), WO 2014100158 A1 20140626. 2. W Reinisch, et al. P568 An open-label, multicenter, phase ib, pharmacokinetic (pk) and safety study of a fimh blocker, Sibofimloc (TAK-018/EB8018), in patients with Crohn’s disease (CD), Journal of Crohn's and Colitis, Volume 14, Issue Supplement_1, January 2020: S479–S480. |
| 溶解性： |
Soluble in DMSO |
| 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 |
1.539 ml |
7.696 ml |
15.392 ml |
| 5 mM |
0.308 ml |
1.539 ml |
3.078 ml |
| 10 mM |
0.154 ml |
0.77 ml |
1.539 ml |
| 50 mM |
0.031 ml |
0.154 ml |
0.308 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