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GSK2330672 99%

GSK2330672

源葉(MedMol)
S82917
1345982-69-5
C28H38N2O7S
546.6755
品牌 貨號 產品規格 價格(RMB) 庫存（上海） 北京 武漢 南京 購買數量
源葉(MedMol) S82917-1mg 99% ￥800.00元 5 - - -
源葉(MedMol) S82917-5mg 99% ￥2240.00元 6 - - -
源葉(MedMol) S82917-10mg 99% ￥3600.00元 5 - - -
源葉(MedMol) S82917-50mg 99% ￥10400.00元 預計交期：2-3天 - - -
源葉(MedMol) S82917-100mg 99% ￥14400.00元 預計交期：2-3天 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

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
產品描述： 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
靶點： IC50: 42 nM (Apical sodium-dependent bile acid transporter (ASBT));HBV
體外研究：
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
體內研究：
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.
參考文獻：
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
保存條件： -20℃
配置溶液濃度參考：
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
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參考文獻

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摩爾濃度計算器

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