Linerixibat (Synonyms: GSK2330672)

Name: Linerixibat
Brand: MedChemExpress
SKU: HY-16643
Rating: 5.0 (13 reviews)

Cat. No.: HY-16643 Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Linerixibat Chemical Structure

CAS No. : 1345982-69-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 325	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 325	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1440	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2160	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 13 publication(s) in Google Scholar

11 Publications Citing Use of MCE Linerixibat

: 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.

: 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.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

Clinical Trial

Molecular Weight

546.68

Formula

C₂₈H₃₈N₂O₇S

CAS No.

1345982-69-5

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (282 KB) SDS (538 KB)

COA (258 KB) LCMS (106 KB)

Handling Instructions (2659 KB)

References

[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.

Complete Stock Solution Preparation Table

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

Linerixibat Related Classifications

Metabolic Disease Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Linerixibat (Synonyms: GSK2330672)

Customer Review

Linerixibat Related Antibodies

11 Publications Citing Use of MCE Linerixibat

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Linerixibat Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Linerixibat Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report