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Cat. No. Name Size Price Add Cart
KI0696Glyburide50 mg$155.2

Chemical Characteristic

Product NameGlyburide
SynonymsGlibenclamide
CAS No.10238-21-8
Molecular Weight 494
FormulaC23H28ClN3O5S
Chemical Structure

Biological activities

Glyburide is an ATP-dependent K+ channel (Kir6, KATP) and cystic fibrosis transmembrane conductance regulator (CFTR) Cl- channel blocker. The IC50 value of glyburide against KATP channel is 3.0 nM.[1] Glyburide inhibits recombinant CFTR Cl- channels with an IC50 of 20 µM.[2] In vitro, glyburide inhibits the stimulation by cromakalim and diazoxide of 86Rb+ efflux from the portal vein and aorta with an IC50 of approximately 0.1 µM.[3] In freshly isolated rat islets, maximally effective concentrations of glyburide in stimulating insulin secretion in the presence of 15 mM glucose is 10 µM. At 5 nM glucose, glyburide also increases insulin secretion. Relative to the vehicle control group, glyburide administation (1 mg/kg orally) induces a sustained 2.4- and 1.7-fold increase in plasma insulin concentration in fasted and fed rats, respectively. Glyburide administation (1 mg/kg orally) also induces a 50% decrease in plasma glucose in both fasted and fed rats in vivo.[4] In isolated guinea pig hearts, 1 µM glyburide reduces reactive hyperemia with a peak flow reduction of 30.7% and debt repayment reduction of 78.0%, relative to vehicle-treated hearts. Besides, glyburide treatment (3 mg/kg) also inhibits both the peak flow and the percentage of debt repayment of reactive hyperemia in dogs.[5]

Protocols

In vivo: Glyburide is dissolved in 100% PEG 400 with heat in a water bath for 10 minutes.[5]

References

[1] Mukai E, et al. Metabolic inhibition impairs ATP-sensitive K+ channel block by sulfonylurea in pancreatic beta-cells. Am J Physiol. 1998, 274(1 Pt 1): E38-44.
[2] Sheppard DN, et al. Effect of ATP-sensitive K+ channel regulators on cystic fibrosis transmembrane conductance regulator chloride currents. J Gen Physiol. 1992, 100(4): 573-591.
[3] Quast U, et al. In vitro and in vivo comparison of two K+ channel openers, diazoxide and cromakalim, and their inhibition by glibenclamide. J Pharmacol Exp Ther. 1989, 250(1): 261-271. 閵嗏偓閵嗏偓
[4] Hargrove DM, et al. Comparison of the glucose dependency of glucagon-like peptide-1 (7-37) and glyburide in vitro and in vivo. Metabolism. 1996, 45(3): 404-409. 閵嗏偓閵嗏偓
[5] Clayton FC, et al. Coronary reactive hyperemia and adenosine-induced vasodilation are mediated partially by a glyburide-sensitive mechanism. Pharmacology. 1992, 44(2): 92-100. 閵嗏偓閵嗏偓

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