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Gliclazide

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Chemical Structure| 21187-98-4 同义名 : S1702;SE1702;S-852;Diaikron;Nordialex;Glimicron;Diamicron
CAS号 : 21187-98-4
货号 : A604981
分子式 : C15H21N3O3S
纯度 : 98%
分子量 : 323.411
MDL号 : MFCD00409893
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(324.66 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Potassium Channel

    Potassium channel, IC50:184 nM
描述 Potassium (K) channel, or the ATP-sensitive potassium channel, is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The potassium channel plays a major role in controlling the beta-cell membrane potential and thereby insulin release. Gliclazide is an ATP-sensitive potassium channel blocker. In an experimental system, potassium channel activities of cloned beta-cells were measured by recording macroscopic currents in giant inside-out membrane patches. The results showed that gliclazide inhibited beta-cell K (ATP) channels at two sites: a high-affinity site, which is half-maximally blocked (Ki) at 50 nM and a low-affinity site with a Ki of 3 mM. In the other hand, cloned cardiac and smooth muscle K(ATP) channels did not show high-affinity block by gliclazide[3]. According to another report, Gliclazide blocked whole-cell beta-cell KATP currents with an IC50 of 184 nM but was much less effective in cardiac and smooth muscle, with IC50s of 19.5 μM and 37.9 μM, respectively[4]. In an experiment assessing the protective effect of gliclazide on 3T3L1 adipocytes from insulin resistance induced by oxidative stress, it was found that addition of 0.1 to 10 μM gliclazide to hydrogen peroxide-treated cells dose-dependently restored glucose uptake, with 5 μM gliclazide significantly restoring glucose uptake to 93.3 ± 6.6% even under hydrogen peroxide, while the data of the corresponding control group was 65.9 ± 7.8%[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.09mL

0.62mL

0.31mL

15.46mL

3.09mL

1.55mL

30.92mL

6.18mL

3.09mL
参考文献

[1]Shimoyama T, Yamaguchi S, et al. Gliclazide protects 3T3L1 adipocytes against insulin resistance induced by hydrogen peroxide with restoration of GLUT4 translocation. Metabolism. 2006 Jun;55(6):722-30.

[2]Lawrence CL, Proks P, 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 Aug;44(8):1019-25.

[3]Gribble FM, Ashcroft FM. Differential sensitivity of beta-cell and extrapancreatic K(ATP) channels to gliclazide. Diabetologia. 1999 Jul;42(7):845-8.

[4]Lawrence CL, Proks P, Rodrigo GC, Jones P, Hayabuchi Y, Standen NB, Ashcroft FM. 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 Aug;44(8):1019-25.

[5]Shimoyama T, Yamaguchi S, Takahashi K, Katsuta H, Ito E, Seki H, Ushikawa K, Katahira H, Yoshimoto K, Ohno H, Nagamatsu S, Ishida H. Gliclazide protects 3T3L1 adipocytes against insulin resistance induced by hydrogen peroxide with restoration of GLUT4 translocation. Metabolism. 2006 Jun;55(6):722-30.