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Gliclazide (Diamicron) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 ?30 nM. Gliclazide (Diamicron) binds to sulfonylurea receptors on the surface of the Beta islet cells found in the pancreas. This binding effectively closes the K+ ion channels. This decreases the efflux of potassium from the cell which leads to the depolarization of the cell. This causes voltage dependent Ca2+ ion channels to open increasing the Ca2+ influx. The calcium can then bind to and activate calmodulin which in turn leads to exocystosis of insulin vesicles leading to insulin release. Gliclazide is used for control of hyperglycemia in gliclazide-responsive diabetes mellitus of stable, mild, non-ketosis prone, maturity-onset or adult type. Gliclazide (Diamicron) is used when diabetes cannot be controlled by proper dietary management and exercise or when insulin therapy is not appropriate.
| Molecular Weight | 323.41 |
| Formula | C15H21N3O3S |
| CAS Number | 21187-98-4 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Marwah Aljohani, et al. Dual-drug amorphous formulation of gliclazide
[2] Fatmah A M Al-Omary. Gliclazide
[3] Awadhesh Kumar Singh, et al. Is gliclazide a sulfonylurea with difference? A review in 2016
| Related Potassium Channel Products |
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| TAK-438
TAK-438 is a novel and potent potassium-competitive acid blocker (P-CAB) with IC50 of 19 nM. |
| ML133 hydrochloride
ML133 hydrochloride is a selective inhibitor of the Kir2 family of inward rectifier (IRK, KCNJ) potassium channels. |
| Doxapram hydrochloride hydrate
Doxapram hydrochloride hydrate inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively. |
| Gliquidone
Gliquidone is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM. |
| Pinacidil monohydrate
Pinacidil monohydrate is known to augment a time-independent outward current in cardiac tissues by activating the ATP-regulated potassium channels. |
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