GSK1292263
Modify Date: 2024-01-15 09:27:35
GSK1292263 structure
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Common Name | GSK1292263 | ||
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| CAS Number | 1032823-75-8 | Molecular Weight | 456.558 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 655.1±65.0 °C at 760 mmHg | |
| Molecular Formula | C23H28N4O4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 350.0±34.3 °C | |
Use of GSK1292263GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes.IC50 value:Target: GPR119in 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: 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]. |
| Name | 5-[4-[[6-(4-methylsulfonylphenyl)pyridin-3-yl]oxymethyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole |
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| Synonym | More Synonyms |
| Description | GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes.IC50 value:Target: GPR119in 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: 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]. |
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| Related Catalog | |
| References |
[2]. Brown KK, et al. Diabetes, 2010, 59(Suppl. 1), Abst 1733-P. |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 655.1±65.0 °C at 760 mmHg |
| Molecular Formula | C23H28N4O4S |
| Molecular Weight | 456.558 |
| Flash Point | 350.0±34.3 °C |
| Exact Mass | 456.183136 |
| PSA | 106.80000 |
| LogP | 1.67 |
| Vapour Pressure | 0.0±2.0 mmHg at 25°C |
| Index of Refraction | 1.565 |
| Storage condition | -20℃ |
|
~85%
GSK1292263 CAS#:1032823-75-8 |
| Literature: US2010/29650 A1, ; Page/Page column 50 ; |
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~%
GSK1292263 CAS#:1032823-75-8 |
| Literature: US2010/29650 A1, ; Page/Page column 82 ; |
![{1-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl}methanol structure](https://www.chemsrc.com/caspic/447/1032824-92-2.png)
| Precursor 3 | |
|---|---|
| DownStream 0 | |
| 5-{[1-(3-Isopropyl-1,2,4-oxadiazol-5-yl)-4-piperidinyl]methoxy}-2-[4-(methylsulfonyl)phenyl]pyridine |
| Pyridine, 5-[[1-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl]methoxy]-2-[4-(methylsulfonyl)phenyl]- |
| GSK1292263 |
| 3-Isopropyl-5-(4-(((6-(4-(methylsulfonyl)phenyl)pyridin-3-yl)oxy)methyl)piperidin-1-yl)-1,2,4-oxadiazole |