Art. -Nr.: HY-16643

Linerixibat

Name: Linerixibat
Brand: MedChemExpress
SKU: HY-16643
Price: 100.00 USD
Availability: InStock
Rating: 5 (13 reviews)

(Synonyms: GSK2330672)

13 Cited Publications

Kundenbewertung

Based on 13 publication(s) in Google Scholar

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.88%
CAS. Nr.: 1345982-69-5
Formel: C₂₈H₃₈N₂O₇S
Molecular Weight:546.68

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Linerixibat Chemical Structure

CAS. Nr.: 1345982-69-5

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 42 nM (Apical sodium-dependent bile acid transporter (ASBT))^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	1.9 nM Compound: 56, GSK2330672	Inhibition of rat ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis Inhibition of rat ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	[PMID: 23678871]
HEK293	IC₅₀	2.1 nM Compound: 56, GSK2330672	Inhibition of mouse ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis Inhibition of mouse ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	[PMID: 23678871]
HEK293	IC₅₀	42 nM Compound: 56, GSK2330672	Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	[PMID: 23678871]

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Zucker Diabetic Fatty (ZDF) rat^[1]
Dosage:

0.05 mg/kg, 0.1 mg/kg, 0.5 mg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg
Administration:

Oral gavage; twice daily; for 14 days
Result:

Led to a 1.30-1.64% reduction in hemoglobin A1c (HbA1c), a greater than 50% reduction in nonfasted plasma glucose to below 200 mg/dL, and statistically significant higher plasma insulin.

Related Protocols :

Research Protocol for Metabolic Diseases

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1345982-69-5
Appearance Solid
Molecular Weight 546.68
Formel C₂₈H₃₈N₂O₇S
Color White to off-white
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
Synonyms

GSK2330672
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (13)

All WB

Sort by:

Journal Impact Factor

Nat Commun

An FGF15/19-TFEB regulatory loop controls hepatic cholesterol and bile acid homeostasis. [Abstract]

2020 Jul 17;11(1):3612. PMID: 32681035

Linerixibat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Jul 17;11(1):3612. [Abstract]

TFEB protein in total liver lysates and nuclear fractions. GSK2330672 (GSK) treatment significantly increases hepatic TFEB nuclear abundance without altering total hepatic TFEB mRNA or protein in mice.
Gut Microbes

Dietary cholesterol impairs cognition via gut microbiota-derived deoxycholic acid in obese mice. [Abstract]

2025 Dec;17(1):2537753. PMID: 40717663
Sci Adv

Noninvasive imaging and quantification of bile salt hydrolase activity: From bacteria to humans. [Abstract]

2021 Feb 3;7(6):eaaz9857. PMID: 33536224
JHEP Rep

Combined inhibition of bile salt synthesis and intestinal uptake reduces cholestatic liver damage and colonic bile salts in mice. [Abstract]

2023 Sep 25;6(1):100917. PMID: 38074508
Cell Mol Gastroenterol Hepatol

Combined ASBT Inhibitor and FGF15 Treatment Improves Therapeutic Efficacy in Experimental Nonalcoholic Steatohepatitis. [Abstract]

2021;12(3):1001-1019. PMID: 33965587
Cell Rep

Polystyrene nanoplastics readily penetrate intestine and cause sex-specific effects mediated by bile acids and microbiome. [Abstract]

2026 Jan 22;45(2):116859. PMID: 41575856
Food Funct

Sargassum fusiforme fucoidan alleviates diet-induced insulin resistance by inhibiting colon-derived ceramide biosynthesis. [Abstract]

2021 Sep 20;12(18):8440-8453. PMID: 34374401
J Lipid Res

Combining ASBT inhibitor and FGF15 treatments enhances therapeutic efficacy against cholangiopathy in female but not male Cyp2c70 knockout mice. [Abstract]

2023 Mar;64(3):100340. PMID: 36737039
Liver Res

Effects of apical sodium-bile acid transporter inhibitor and obeticholic acid co-treatment in experimental non-alcoholic steatohepatitis. [Abstract]

2022 Dec;6(4):276-283. PMID: 36819659
Cell Microbiol

Bile acid and bile acid transporters are involved in the pathogenesis of acute hepatopancreatic necrosis disease in white shrimp Litopenaeus vannamei. [Abstract]

2020 Jan;22(1):e13127. PMID: 31610617
Alcohol Clin Exp Res

Gut-restricted apical sodium-dependent bile acid transporter inhibitor attenuates alcohol-induced liver steatosis and injury in mice. [Abstract]

2021 Jun;45(6):1188-1199. PMID: 33885179
Biomed Pharmacother

Studies on absorption mechanism and pharmacokinetic properties of albendazole-bile acid conjugate: In vivo and in vitro. [Abstract]

2024 Oct:179:117400. PMID: 39243427
Gene Expr

HNF4α Regulates CSAD to Couple Hepatic Taurine Production to Bile Acid Synthesis in Mice. [Abstract]

2018 Aug 22;18(3):187-196. PMID: 29871716

Linerixibat purchased from MedChemExpress. Usage Cited in: Gene Expr. 2018 Aug 22;18(3):187-196. [Abstract]

Hepatic cysteine sulfinic acid decarboxylase (CSAD) protein are significantly increased in mice treated with GSK672.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (91.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8292 mL

9.1461 mL

18.2922 mL

5 mM

0.3658 mL

1.8292 mL

3.6584 mL

10 mM

0.1829 mL

0.9146 mL

1.8292 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (4.57 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (538 KB)
- English - EN (538 KB)
- Français - FR (538 KB)
- Deutsch - DE (538 KB)
- Norwegian - NO (538 KB)
- Español - ES (538 KB)
- Swedish - SV (538 KB)
- Italian - IT (538 KB)
- Korean - KR (538 KB)
- Portuguese - PT (538 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8292 mL	9.1461 mL	18.2922 mL	45.7306 mL
	5 mM	0.3658 mL	1.8292 mL	3.6584 mL	9.1461 mL
	10 mM	0.1829 mL	0.9146 mL	1.8292 mL	4.5731 mL
	15 mM	0.1219 mL	0.6097 mL	1.2195 mL	3.0487 mL
	20 mM	0.0915 mL	0.4573 mL	0.9146 mL	2.2865 mL
	25 mM	0.0732 mL	0.3658 mL	0.7317 mL	1.8292 mL
	30 mM	0.0610 mL	0.3049 mL	0.6097 mL	1.5244 mL
	40 mM	0.0457 mL	0.2287 mL	0.4573 mL	1.1433 mL
	50 mM	0.0366 mL	0.1829 mL	0.3658 mL	0.9146 mL
	60 mM	0.0305 mL	0.1524 mL	0.3049 mL	0.7622 mL
	80 mM	0.0229 mL	0.1143 mL	0.2287 mL	0.5716 mL

Bioz

Linerixibat

13 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Linerixibat

Publications Citing Use of MedChemExpress (MCE) Linerixibat