Home Endocrinology & Hormones GPR agonist GSK1292263 For research use only.

GSK1292263

GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.

GSK1292263 Chemical Structure

GSK1292263 Chemical Structure

CAS: 1032823-75-8

Selleck's GSK1292263 has been cited by 1 Publication

1 Customer Review

Purity & Quality Control

Batch: S214901 DMSO] 34 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.66%
99.66

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Biological Activity

Description GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.
Targets
GPR119 [1]
In vitro
In vitro GSK-1292263 is selected from 1538 compounds by using Hypo1, the Fit-Value and Estimate of GSK-1292263 that is aligned in Hypo1 are 8.8 and 7.7 (nM), respectively. [1]
In Vivo
In vivo GSK-1292263 administrated at a single dose of 3-30 mg/kg in the absence of nutrients correlates with increased levels of circulating gastrointestinal peptides, including glucagon-like peptide 1 (GLP-1), gastric inhibitory polypeptide (GIP), peptide YY (PYY) and glucagon in male Sprague-Dawley rats, the increase is enhanced following administration of glucose in the oral glucose tolerance test (OGTT). GSK-129226 significant increases in the peak insulin response and insulin AUC(0-15 min) of 30-60% compared with values in the vehicle control cohort in the intravenous glucose tolerance test in rats, this insulin upregulation correlated with a significant increase in the glucose disposal rate. GSK-1292263 is associated with a statistically significant increase in insulin immunoreactivity in pancreatic sections in a 6-week study performed in Zucker diabetic fatty rats, compared with insulin immunoreactivity in samples obtained from rats receiving vehicle control. GSK-1292263 administrated at dose of 10 or 30 mg/kg or vehicle control at 2 hours prior to insulin infusion in hyperinsulinemic-euglycemic clamps stimulates glucagon secretion without increasing blood glucose levels Sprague-Dawley rats. [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01101568 Completed
Diabetes Mellitus Type 2
GlaxoSmithKline
 April 14 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 456.56 Formula

C23H28N4O4S
CAS No. 1032823-75-8 SDF Download GSK1292263 SDF
Smiles CC(C)C1=NOC(=N1)N2CCC(CC2)COC3=CN=C(C=C3)C4=CC=C(C=C4)S(=O)(=O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 34 mg/mL ( (74.46 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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