GSK1292263 - 10mM in DMSO , Glucose-dependent insulinotropic receptor agonist, CAS No.1032823-75-8, Glucose-dependent insulinotropic receptor agonist

CAS: 1032823-75-8 Cat. No.: G408680 Molecular Weight: 456.56

GRADE & PURITY 10mM in DMSO

Synonyms

5-((1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)methoxy)-2-(4-(methylsulfonyl)phenyl)pyridine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

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

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 Glukagon-like peptide 1 (GLP-1), gastric inhibitory polypeptide (GIP), peptide YY (PYY) and Glukagon 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 Glukagon secretion without increasing blood glucose levels Sprague-Dawley rats.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

5-((1-(3-isopropyl-1, 2, 4-oxadiazol-5-yl)piperidin-4-yl)methoxy)-2-(4-(methylsulfonyl)phenyl)pyridine

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

AGONIST

Mechanism of action

Glucose-dependent insulinotropic receptor agonist

Product Properties

• ALogP: 4

Names and Identifiers

• Isomeric SMILES: CC(C)C1=NOC(=N1)N2CCC(CC2)COC3=CN=C(C=C3)C4=CC=C(C=C4)S(=O)(=O)C
• Molecular Weight: 456.56
• Reaxy-Rn: 19915189
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=19915189&ln=

Associated Targets(Human)

GPR119 Tclin Glucose-dependent insulinotropic receptor (1 Activities)

Discover Target: GPR119

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)