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Gliclazide

CAS No. : 21187-98-4

MCE 国际站：Gliclazide

产品活性：Gliclazide (S1702) 是全细胞的 β 细胞 ATP 敏感型钾流 (potassium currents) 阻断剂，IC₅₀ 为 184 nM，用作降糖药。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

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.

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