Art. -Nr.: HY-12066

GSK1292263

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

GSK-1292263 is an orally available GPR119 agonist with pEC₅₀s of 6.9 and 6.7 for human and rat GPR119, respectively. GSK-1292263 can be used for the research of type 2 diabetes mellitus (T2DM).

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Reinheit: 98.68%
CAS. Nr.: 1032823-75-8
Formel: C₂₃H₂₈N₄O₄S
Molecular Weight:456.56

Speicherung:

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

GSK1292263 Chemical Structure

CAS. Nr.: 1032823-75-8

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vivo

GSK1292263 upregulates glucagon-like peptide-1 and enhances glucose-dependent insulin secretion and improves glucose homeostasis in type 2 diabetic rats^[2].

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

Animal Model:

Male neonatal Streptozotocin (STZ)-induced SD rats (7 weeks of age)^[2]
Dosage:

30 mg/kg
Administration:

Orally given; once a day for 2 weeks
Result:

The AUC of plasma glucose (AUC_PG) in the single treatment of the GSK1292263 group was numerically lower than that of the vehicle group, but the effect was modest.

Clinical Trial

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

Chemical Information

CAS. Nr. 1032823-75-8
Appearance Solid
Molecular Weight 456.56
Formel C₂₃H₂₈N₄O₄S
Color White to off-white
SMILES

CC(C1=NOC(N2CCC(CC2)COC3=CN=C(C=C3)C4=CC=C(C=C4)S(C)(=O)=O)=N1)C
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 (7)

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Journal Impact Factor

Nat Chem

Activity of GPCR-targeted drugs influenced by human gut microbiota metabolism. [Abstract]

2025 Apr 3. PMID: 40181149
J Exp Clin Cancer Res

GPR119 agonist enhances gefitinib responsiveness through lactate-mediated inhibition of autophagy. [Abstract]

2018 Nov 29;37(1):295. PMID: 30497501
J Ethnopharmacol

Tianwang Buxin Decoction ameliorates neuroinflammation in insomnia via adenosine accumulation-mediated AMPK/SIRT1 pathway. [Abstract]

2026 Apr 30:121790. PMID: 42069163
Biomol Ther (Seoul)

A Novel Anti-Fibrotic Role of G-Protein-Coupled Receptor 119 in Hepatic Stellate Cells. [Abstract]

2026 May 1;34(3):666-675. PMID: 42059036
FASEB J

GPR119: a promising target for nonalcoholic fatty liver disease. [Abstract]

2016 Jan;30(1):324-35. PMID: 26399788

GSK1292263 purchased from MedChemExpress. Usage Cited in: FASEB J. 2016 Jan;30(1):324-35. [Abstract]

Treatment with 2 synthetic GPR119 agonists, MBX-2982 (MBX) and GSK1292263 (GSK), suppresses T090-induced SREBP-1 expression and mRNA levels of SREBP-1 target genes such as FAS, ACC, and SCD-1.
bioRxiv

2025 Oct 17.
College of Pharmacy

Seoul National University. 2015 Aug.

GSK1292263 purchased from MedChemExpress. Usage Cited in: College of Pharmacy. Seoul National University. 2015 Aug.

Effects of GPR119 ligands on T090-induced pSREBP-1 and lipogenic enzymes expression. Primary cultured hepatocytes from GPR119-WT and -KO mice and HepG2 cells are pretreated with two GPR119 ligands [(MBX (MBX-2982) or GSK (GSK1292263)] for 30 min and the cells are exposed to T090 for 12 h.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 20 mg/mL (43.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.1903 mL

10.9515 mL

21.9029 mL

5 mM

0.4381 mL

2.1903 mL

4.3806 mL

10 mM

0.2190 mL

1.0951 mL

2.1903 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 90% Corn Oil

Solubility: ≥ 2 mg/mL (4.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2 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 (20.0 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 (273 KB)
SDS (596 KB)
- English - EN (596 KB)
- Français - FR (596 KB)
- Deutsch - DE (596 KB)
- Norwegian - NO (596 KB)
- Español - ES (596 KB)
- Swedish - SV (596 KB)
- Italian - IT (596 KB)
- Korean - KR (596 KB)
- Portuguese - PT (596 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]. X. Zhu, et al. GPR119 Agonists: A Novel Strategy for Type 2 Diabetes Treatment.

[2]. Koji Matsumoto, et al. DS-8500a, an Orally Available G Protein-Coupled Receptor 119 Agonist, Upregulates Glucagon-Like Peptide-1 and Enhances Glucose-Dependent Insulin Secretion and Improves Glucose Homeostasis in Type 2 Diabetic Rats. J Pharmacol Exp Ther. 2018 Dec;367(3):509-517. [Content Brief]

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	2.1903 mL	10.9515 mL	21.9029 mL	54.7573 mL
	5 mM	0.4381 mL	2.1903 mL	4.3806 mL	10.9515 mL
	10 mM	0.2190 mL	1.0951 mL	2.1903 mL	5.4757 mL
	15 mM	0.1460 mL	0.7301 mL	1.4602 mL	3.6505 mL
	20 mM	0.1095 mL	0.5476 mL	1.0951 mL	2.7379 mL
	25 mM	0.0876 mL	0.4381 mL	0.8761 mL	2.1903 mL
	30 mM	0.0730 mL	0.3650 mL	0.7301 mL	1.8252 mL
	40 mM	0.0548 mL	0.2738 mL	0.5476 mL	1.3689 mL

Keywords

GSK1292263

7 Cited Publications

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GSK1292263

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Orally Active Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK1292263

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK1292263

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Orally Active Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK1292263

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK1292263 Related Classifications

HY-12066 Related Classifications