Name | Ingliforib; CP 368296 GPi 296 |
Synonyms | 296 CP296 CP 296 CP-296 CPD2802 GPi 296 CP368296 CP 368296 CP-368296 Ingliforib; CP 368296 |
CAS | 186392-65-4 |
Molecular Formula | C23H24ClN3O5 |
Molar Mass | 457.91 |
Density | 1.495±0.06 g/cm3(Predicted) |
Melting Point | 238 °C |
Boling Point | 843.3±65.0 °C(Predicted) |
Solubility | DMSO : 130 mg/mL (283.90 mM; Need ultrasonic) |
pKa | 12.88±0.20(Predicted) |
Storage Condition | -20°C |
In vitro study | Ingliforib is a glycogen phosphorylase inhibitor, and inhibits the myocardial GP isoforms (muscle and brain) with IC 50 s of 352 and 150 nM, respectively, also a potent inhibitor of the liver isoform (IC 50 of 52 nM). Ingliforib (0.1, 1, 10 μM) dose-dependently reduces infarct size in the isolated rabbit hearts. |
In vivo study | Ingliforib (15 mg/kg) potently reduces infarct size by 52%, and decreases plasma glucose and lactate concentrations in openchest anesthetized rabbits. Ingliforib (15 mg/kg) also inhibits myocardial glycogen phosphorylase a (GPa) and total glycogen phosphorylase (GP) activity in anesthetized rabbits. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.184 ml | 10.919 ml | 21.838 ml |
5 mM | 0.437 ml | 2.184 ml | 4.368 ml |
10 mM | 0.218 ml | 1.092 ml | 2.184 ml |
5 mM | 0.044 ml | 0.218 ml | 0.437 ml |
biological activity | Ingliforib is a glycogen phosphophylase inhibitor, the IC50 values of muscle and brain glycogen phosporylase are 52,352 and 150 nM, respectively, which has cardioprotective effect. |
Target | IC50: 52 nM, 352 nM, 150 nM (Barin Glycogen phosphor) |