Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can also induce autophagy.
Glibenclamide (2 mg/kg; p.o.) increases of insulin release and rapid drop of blood glucose level in mice.
| Molecular Weight | 494 |
| Formula | C23H28ClN3O5S |
| CAS Number | 10238-21-8 |
| Solubility (25°C) | DMSO > 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Żaneta Kimber-Trojnar, et al. Is glyburide safe in pregnancy?
[4] L P Krall. Glyburide (DiaBeta): a new second-generation hypoglycemic agent
[5] G F Peart, et al. The metabolism of glyburide in subjects of known debrisoquin phenotype
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