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Linerixibat

Synonyms: GSK2330672

Linerixibat (GSK 2330672, GSK 672), a highly potent, nonabsorbable inhibitor of apical sodium dependent bile acid transporter (ABST), also known as the ileal bile acid transporter (IBAT), is used to the treatment of cholestatic pruritus in primary biliary Cholangitis. The IC50 of human ASBT is 42 nM.

Linerixibat Chemical Structure

Linerixibat Chemical Structure

CAS: 1345982-69-5

Purity & Quality Control

Batch: S352901 DMSO] 50 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.99%
99.99

Linerixibat Related Products

Biological Activity

Description Linerixibat (GSK 2330672, GSK 672), a highly potent, nonabsorbable inhibitor of apical sodium dependent bile acid transporter (ABST), also known as the ileal bile acid transporter (IBAT), is used to the treatment of cholestatic pruritus in primary biliary Cholangitis. The IC50 of human ASBT is 42 nM.
In vitro
In vitro

The zwitterionic, nonhygroscopic, crystalline salt form of Linerixibat shows good aqueous solubility at pH 7.4 (>7 mg/mL), excellent thermal stability, and does not generate reactive or humanspecific metabolite, characteristics.[3]
Cell Research Cell lines Human Multi-Drug Resistance 1-Madin-Darby Canine Kidney (HMDR1-) cells
Concentrations 3 μM
Incubation Time 30 min
Method

HMDR1-MDCK cells are seeded at 6.6 × 105 cells/well onto 12-well polycarbonate Transwells filter membranes with 0.4 μm pore size. After three days, media is removed from both the apical and basolateral chambers and replaced with transport buffer (HBSS containing 25 mM glucose and 25 mM HEPES) containing the P-gp inhibitor GF120918A at a final concentration of 2 μM. After a 30 min equilibration, the transport buffer is removed from the apical chambers and replaced with fastedstate simulated intestinal fluid containing 3 μM Linerixibat, 2 μM GF120918A, 25 mM glucose, and 250 μM Lucifer Yellow CH. Next, the transport buffer is removed from the basolateral chambers and replaced with transport buffer containing 1% (w/v) human serum albumin and 2 μM GF120918A. After 60 min incubation at 37 °C, samples are collected from the apical (donor) and basolateral (receiver) compartments and added to acetonitrile (1:1 and 1:2 (v/v), respectively). Receiver samples are then centrifuged and the supernatants are removed and analyzed by LC-MS/MS.
In Vivo
In vivo

Linerixibat (twice daily; for 14 days) treatment lowers glucose in an animal model of type 2 diabetes.[3]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05435170 Completed
Pruritus
GlaxoSmithKline
 August 11 2022 Phase 1
NCT05393076 Completed
Pruritus
GlaxoSmithKline
 July 19 2022 Phase 1
NCT04053023 Completed
Cholestasis
GlaxoSmithKline
 August 27 2019 Phase 1
NCT02966834 Completed
Cholestasis
GlaxoSmithKline
 January 11 2017 Phase 2
NCT02801981 Completed
Cholestasis
GlaxoSmithKline
 June 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 546.68 Formula

C28H38N2O7S
CAS No. 1345982-69-5 SDF --
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 50 mg/mL ( (91.46 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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