Gliclazide

Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. (In Vitro) :Gliclazide (S1702) further characterize its mechanism of hypoglycemic effect: the observed improvements in insulin sensitivity and in GLUT4 translocation indicate that gliclazide counters the hydrogen peroxide-induced insulin resistance in 3T3L1 adipocytes and also would further augment the hypoglycemic effect of this drug as insulinotropic sulfonylurea.Gliclazide blocked whole-cell beta-cell KATP currents with an IC50 of 184 +/- 30 nmol/l (n=6-10) but was much less effective in cardiac and smooth muscle (IC50s of 19.5 +/- 5.4 micromol/l (n=6-12) and 37.9 +/- 1.0 micromol/l (n=5-10), respectively) . In all three tissues, the action of the drug on whole-cell KATP currents was rapidly reversible. In inside-out patches on beta-cells, gliclazide (1 micromol/l) produced a maximum of 66 +/- 13 % inhibition (n=5), compared with more than 98 % block in the whole-cell configuration. Gliclazide is a high-potency sulphonylurea which shows specificity for the pancreatic beta-cell KATP channel over heart and smooth muscle. In this respect, it differs from glibenclamide.

21187-98-4

Gliclazide | Diamicron | Glimicron | Nordialex | Diaikron | S-1702 | S-852

Pharmacology & Drug Discovery

>98% (HPLC)

DMSO: 65 mg/mL (200.98 mM)

CC1=CC=C (C=C1) S (=O) (=O) NC (=O) NN2CC3CCCC3C2

C15H21N3O3S

323.42

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.