Linerixibat

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[1][2][3].

Product Specifications

CAS Number

[1345982-69-5]

Product Name Alternative

GSK2330672

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335, H401, H411

Target

Apical Sodium-Dependent Bile Acid Transporter

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/GSK2330672.html

Purity

99.88

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(O)CC(NCC1=C(OC)C=C(C2=C1)[C@@H](C3=CC=CC=C3)N[C@](CC)(CCCC)CS2(=O)=O)CC(O)=O

Molecular Formula

C28H38N2O7S

Molecular Weight

546.68

Precautions

H302, H315, H319, H335, H401, H411

References & Citations

[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]Linerixibat (GSK2330672) granted Orphan Status. September 24, 2019.|[3]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.