Gliclazide|cas 21187-98-4|Supplied by DC Chem

Cas No.:	21187-98-4
SMILES:	O=C(NS(C1=CC=C(C)C=C1)(=O)=O)NN2CC(CCC3)C3C2
Formula:	C₁₅H₂₁N₃O₃S
M.Wt:	323.41
Purity:	>98%, Standard References Grade
Sotrage:	4°C for 1 year, -20°C for more than 2 years

Description:

Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.Target: Potassium Channelgliclazide 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 [1]. 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 [2].

References:

[1]. Shimoyama, T., et al., Gliclazide protects 3T3L1 adipocytes against insulin resistance induced by hydrogen peroxide with restoration of GLUT4 translocation. Metabolism, 2006. 55(6): p. 722-30. [2]. Lawrence, C.L., et al., Gliclazide produces high-affinity block of KATP channels in mouse isolated pancreatic beta cells but not rat heart or arterial smooth muscle cells. Diabetologia, 2001. 44(8): p. 1019-25.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101
2018-0101

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