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Linerixibat

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Catalog No. T3978Cas No. 1345982-69-5
Alias Iinerixibat, GSK2330672

Linerixibat (GSK2330672) is a highly effective, nonabsorbable ASBT inhibitor (IC50: 42 ± 3 nM) that can lower glucose in an animal model of type 2 diabetes and demonstrates excellent developability properties.

Linerixibat

Linerixibat

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Purity: 99.98%
Catalog No. T3978Alias Iinerixibat, GSK2330672Cas No. 1345982-69-5
Linerixibat (GSK2330672) is a highly effective, nonabsorbable ASBT inhibitor (IC50: 42 ± 3 nM) that can lower glucose in an animal model of type 2 diabetes and demonstrates excellent developability properties.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$76In StockIn Stock
2 mg$119In StockIn Stock
5 mg$222In StockIn Stock
10 mg$372In StockIn Stock
25 mg$629In StockIn Stock
50 mg$896-In Stock
1 mL x 10 mM (in DMSO)$268In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.98%
Color:White
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Product Introduction

Linerixibat AI Summary
Linerixibat exhibits bioactivities related to the inhibition of ASBT (Apical Sodium-dependent Bile Acid Transporter) and displays antidiabetic properties as well as antiviral activity. It shows potent inhibition of ASBT in rat, mouse, and human cell models with varying IC50 values, leading to increased fecal bile acid excretion and high drug recovery in rat feces. In Zucker diabetic fatty rats, it resulted in reduced non-fasted plasma glucose levels and blood HbA1c levels, demonstrating significant antidiabetic activity. The compound also inhibits taurocholate uptake with an IC50 of 43.0 nM and has favorable aqueous solubility and pharmacokinetic profiles in different animal models. Additionally, Linerixibat exhibits antiviral activity by inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 cells and VERO-6 cells with various inhibition rates and demonstrates SARS-CoV-2 3CL-Pro protease inhibition at 20µM. It also shows inhibitory activity against the human HDAC6 enzyme, suggesting potential as an HDAC6 inhibitor in enzymatic assays..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Linerixibat (GSK2330672) is a highly effective, nonabsorbable ASBT inhibitor (IC50: 42 ± 3 nM) that can lower glucose in an animal model of type 2 diabetes and demonstrates excellent developability properties.
Targets&IC50
ASBT:42 ± 3 nM
SynonymsIinerixibat, GSK2330672
Chemical Properties
Molecular Weight546.68
FormulaC28H38N2O7S
Cas No.1345982-69-5
SmilesCCCC[C@]1(CC)CS(=O)(=O)c2cc(CNC(CC(O)=O)CC(O)=O)c(OC)cc2[C@H](N1)c1ccccc1
Relative Density.1.218 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 21.5 mg/mL (39.33 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8292 mL9.1461 mL18.2922 mL91.4612 mL
5 mM0.3658 mL1.8292 mL3.6584 mL18.2922 mL
10 mM0.1829 mL0.9146 mL1.8292 mL9.1461 mL
20 mM0.0915 mL0.4573 mL0.9146 mL4.5731 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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