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).

Solid

FimH adhesion

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature or refrigerated transportation.

• [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 Crohns and Colitis, Volume 14, Issue Supplement_1, January 2020: S479–S480.

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。