Glycogen Phosphorylase Inhibitor
Glycogen Phosphorylase Inhibitor Basic information
- Product Name:
- Glycogen Phosphorylase Inhibitor
- Synonyms:
-
- Glycogen Phosphorylase Inhibitor
- 2-chloro-4,5-difluoro-N-[[2-methoxy-5-(methylcarbamoylamino)phenyl]carbamoyl]benzamide
- Benzamide, 2-chloro-4,5-difluoro-N-[[[2-methoxy-5-[[(methylamino)carbonyl]amino]phenyl]amino]carbonyl]-
- Glycogen Phosphorylase Inhibitor inhibitor
- Glycogen phosphorylase-IN-1
- CAS:
- 648926-15-2
- MF:
- C17H15ClF2N4O4
- MW:
- 412.78
- Mol File:
- 648926-15-2.mol
Glycogen Phosphorylase Inhibitor Chemical Properties
- Density
- 1.490±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF:5.0(Max Conc. mg/mL);12.11(Max Conc. mM)
DMSO:5.0(Max Conc. mg/mL);12.11(Max Conc. mM) - form
- White powder solid.
- pka
- 8.47±0.46(Predicted)
- color
- white
Glycogen Phosphorylase Inhibitor Usage And Synthesis
Description
Glycogen phosphorylase in the liver, muscle, and brain initiate glycogenolysis by releasing glucose-1-phosphate from glycogen. Glycogen phosphorylase inhibitor is a cell-permeable acyl urea first identified as an inhibitor of human liver glycogen phosphorylase (IC50 = 53 nM). It blocks glucagon-induced hepatic glycogenolysis in vivo. Glycogen phosphorylase inhibitor has been used to study glycogen utilization in human liver HepG2 cells, retinal explants, and human T lymphocyte Kit 225 cells.
Uses
Glycogen Phosphorylase Inhibitor is used in biological studies to evaluate glycogen utilization in human liver HepG2 cells.
in vivo
Glycogen phosphorylase-IN-1 (5 mg/kg, i.v., single dose) inhibits the glycogenolysis in hepatocytes, ameliorates the glucagon stimulated hyperglycemic in wistar rats[1].
| Animal Model: | Glucagon-stimulated hyperglycemic in wistar rats[1] |
| Dosage: | 5 mg/kg |
| Administration: | i.v., single dose |
| Result: | Reduced blood glucose. |
References
[1] THOMAS KLABUNDE. Acyl Ureas as Human Liver Glycogen Phosphorylase Inhibitors for the Treatment of Type 2 Diabetes[J]. Journal of Medicinal Chemistry, 2005, 48 20: 6178-6193. DOI: 10.1021/jm049034y
[2] ALAN CHENG. A role for AGL ubiquitination in the glycogen storage disorders of Lafora and Cori’s disease.[J]. Genes & development, 2007, 21 19: 2399-2409. DOI: 10.1101/gad.1553207
[3] KONSTANTINOS PAPPELIS. The retinal ganglion cells in metabolic syndrome.[J]. Annals of translational medicine, 2024, 12 1: 2. DOI: 10.21037/atm-23-1796
[4] ONETSINE ARRIZABALAGA. Rac1 protein regulates glycogen phosphorylase activation and controls interleukin (IL)-2-dependent T cell proliferation.[J]. The Journal of Biological Chemistry, 2012: 11878-11890. DOI: 10.1074/jbc.m111.297804
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