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GSK1292263

Catalog No. T2701 CAS 1032823-75-8

GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.

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GSK1292263, CAS 1032823-75-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 223.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 531.00
1 mL * 10 mM (in DMSO)	In stock	$ 84.00

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Purity: 99.76%

Purity: 98.34%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.
In vitro	In male Sprague-Dawley rats, GSK-1292263 (3-30 mg/kg) was associated with increased levels of gastrointestinal peptides, including glucagon-like peptide 1, oxyntomodulin, peptide YY, and glucagon, especially in the absence of nutrients. This increase was further enhanced by oral glucose administration during glucose tolerance tests. In a 6-week study on Zucker diabetic fatty rats, GSK-1292263 led to a statistically significant increase in insulin immunoreactivity in pancreatic sections compared to the blank control. Furthermore, in a hyperinsulinemic-normoglycemic clamp experiment in Sprague-Dawley rats, GSK-1292263 (10/30 mg/kg) stimulated glucagon secretion without raising blood glucose levels when administered 2 hours before insulin injection, in comparison to the vehicle control.
In vivo	Utilizing Hypo1, GSK-1292263 was identified from a pool of 1,538 compounds. The Fit-Value of GSK-1292263 corresponding to Hypo1 and its estimated value were 8.8 and 7.7 nM, respectively.
Kinase Assay	FTase and GGTase I Activity Assay: FTase and GGTase I activities from 60,000×g supernatants of human Burkitt lymphoma (Daudi) cells are assayed. Inhibition studies are performed by determining the ability of Ras CAAX peptidomimetics to inhibit the transfer of [3H]farnesyl and [3H]geranylgeranyl from [3H]farnesylpyrophosphate and [3H]geranylgeranylpyrophosphate to H-Ras-CVLS and H-Ras-CVLL, respectively.

Molecular Weight	456.56
Formula	C23H28N4O4S
CAS No.	1032823-75-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 32 mg/mL (70.1 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Zhu X, et al. Eur J Med Chem, 2011, 46(7), 2901-2907.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library GPCR Compound Library Drug Repurposing Compound Library Anti-Diabetic Compound Library Bioactive Compound Library Endocrinology-Hormone Compound Library Clinical Compound Library Bioactive Lipid Compound Library Immunology/Inflammation Compound Library

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Keywords

GSK1292263 1032823-75-8 Endocrinology/Hormones GPCR/G Protein GPR diabetes type mellitus GSK 1292263 GPR119 inhibit G Protein-Coupled Receptor 119 T2DM Inhibitor GSK-1292263 inhibitor

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