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KI0951Glimepiride20 mg$154
Glimepiride50 mg$272

Chemical Characteristic

Product NameGlimepiride
CAS No.93479-97-1
Molecular Weight 490.62
FormulaC24H34N4O5S
Chemical Structure

Biological activities

Glimepiride is a relatively new sulphonylurea used in the treatment of type 2 diabetes. Glimepiride blocks pinacidil-activated whole-cell KATP currents of cardiac myocytes in HEK 293 cells with an IC50 of 6.8 nM. Glimepiride blocks KATP channels formed by co-expression of Kir6.2/SUR2A subunits in HEK 293 cells in outside-out excised patches with an IC50 of 6.2 nM.[1] Glimepiride inhibits Kir6.2/SUR currents by interaction with two sites: a low-affinity site on Kir6.2 with an IC50 of 400 µM and a high- affinity site on SUR (SUR1, SUR2A and SUR2B) with IC50 of 3.0, 5.4 and 7.3 nM. [2] In cultured human coronary arterial endothelial cells, glimepiride inhibits oxidative modification of LDL with an IC50 of 0.88 µM without cytotoxicity. Glimepiride treatment produces significant reduction of atherosclerotic lesions with no significant change observed in levels of plasma lipids. [3]

Protocols

Glimepiride is dissolved in DMSO as stock solution and diluted in Tyrode. [1]

References

[1] Lawrence CL, et al. Effect of metabolic inhibition on glimepiride block of native and cloned cardiac sarcolemmal K(ATP) channels. Br J Pharmacol. 2002, 136(5): 746-752. 閵嗏偓閵嗏偓
[2] Song DK, et al. Glimepiride block of cloned beta-cell, cardiac and smooth muscle K(ATP) channels. Br J Pharmacol. 2001, 133(1): 193-199. 閵嗏偓閵嗏偓
[3] Shakuto S, et al. Glimepiride exhibits prophylactic effect on atherosclerosis in cholesterol-fed rabbits. Atherosclerosis. 2005, 182(2): 209-217. 閵嗏偓閵嗏偓

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