| 产品描述： | Linerixibat (GSK2330672) is a highly potent, nonabsorbable and orally active apical sodium-dependent bile acid transporter (ASBT) inhibitor with an IC50 of 42 nM human ASBT. Linerixibat can be used as lipid-lowering agent. Linerixibat has the potential for type 2 diabetes and Primary Biliary Cholangitis treatment |
| 靶点： |
IC50: 42 nM (Apical sodium-dependent bile acid transporter (ASBT));HBV |
| 体外研究： |
The zwitterionic, nonhygroscopic, crystalline salt form of Linerixibat (Compound 56) shows good aqueous solubility at pH 7.4 (>7 mg/mL), excellent thermal stability, and did not generate reactive or humanspecific metabolite, characteristics |
| 体内研究： |
Linerixibat (GSK2330672; 0.05-10 mg/kg; oral gavage; twice daily; for 14 days; male ZDF rat) treatment lowers glucose in an animal model of type 2 diabetes. Animal Model: Male Zucker Diabetic Fatty (ZDF) rat Dosage: 0.05 mg/kg, 0.1 mg/kg, 0.5 mg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg Administration: Oral gavage; twice daily; for 14 days Result: Led to a 1.30-1.64% reduction in hemoglobin A1c (HbA1c), a greater than 50% reduction in nonfasted plasma glucose to below 200 mg/dL, and statistically significant higher plasma insulin. |
| 参考文献： |
1. Wu Y, et al. Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes. J Med Chem. 2013 Jun 27;56(12):5094-114. 2. Wang Y, et al. HNF4α Regulates CSAD to Couple Hepatic Taurine Production to Bile Acid Synthesis in Mice. Gene Expr. 2018 Aug 22;18(3):187-196. 3. Linerixibat (GSK2330672) granted Orphan Status. September 24, 2019. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.829 ml |
9.146 ml |
18.292 ml |
| 5 mM |
0.366 ml |
1.829 ml |
3.658 ml |
| 10 mM |
0.183 ml |
0.915 ml |
1.829 ml |
| 50 mM |
0.037 ml |
0.183 ml |
0.366 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