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Linerixibat

Name: Linerixibat
Brand: Selleck Chemicals
SKU: S3529
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S3529

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.

Chemical Structure

Molecular Weight: 546.68

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.99

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other Others Inhibitors	Furimazine (PBI 3939) BAY 2927088（Sevabertinib） Guanidinoacetic acid BAPTA-AM Blebbistatin Polybrene (Hexadimethrine Bromide) Silibinin (NSC 651520) Carbazochrome sodium sulfonate (AC-17) Palmitic acid Osthole

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (91.46 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	546.68	Formula	C₂₈H₃₈N₂O₇S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1345982-69-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

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.
In vivo	Linerixibat (twice daily; for 14 days) treatment lowers glucose in an animal model of type 2 diabetes.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23678871/ [2] https://pubmed.ncbi.nlm.nih.gov/32201314/ [3] https://pubmed.ncbi.nlm.nih.gov/23678871/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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