LinerixibatLinerixibat
MedChemExpress (MCE)
HY-16643
1345982-69-5
GSK2330672
99.88%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
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.
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[1].
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[1].
IC50: 42 nM (Apical sodium-dependent bile acid transporter (ASBT))[1] Cellular Effect Cell Line Type Value Description References
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[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. [Content Brief]
[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. [Content Brief]
[3]. Linerixibat (GSK2330672) granted Orphan Status. September 24, 2019.