Diazoxide

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Chemical Structure| 364-98-7 同义名 : 氯甲苯噻嗪 ;Sch-6783; SRG-95213; NSC 76130; NSC 64198; Proglycem
CAS号 : 364-98-7
货号 : A601456
分子式 : C8H7ClN2O2S
纯度 : 95%
分子量 : 230.67
MDL号 : MFCD00078578
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(151.73 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
生物活性
描述 Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment. Diazoxide has powerful protective properties against cardiac ischemia. Diazoxide may have several potential effectors that may potentially contribute to cardioprotection, including KATP channels in the pancreas, smooth muscle, endothelium, neurons and the mitochondrial inner membrane. Diazoxide may also affect other ion channels and ATPases and may directly regulate mitochondrial energetics[3]. Diazoxide is a neuroprotective agent against oxidative stress-induced damage and cellular dysfunction. Diazoxide effectively protects NSC-34 motoneurons from glutamatergic, oxidative and inflammatory damage. Moreover, diazoxide decreased neuronal death in organotypic hippocampal slice cultures after exicitotoxicity and preserved myelin sheath in organotypic cerebellar cultures exposed to pro-inflammatory demyelinating damage[4]. Diazoxide attenuates postresuscitation brain injury, protects mitochondrial function, inhibits brain cell apoptosis, and activates the PKC pathway by opening mitoKATP channels[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.34mL

0.87mL

0.43mL

21.68mL

4.34mL

2.17mL

43.35mL

8.67mL

4.34mL
参考文献

[1]Wu H, Wang P, et al. Diazoxide Attenuates Postresuscitation Brain Injury in a Rat Model of Asphyxial Cardiac Arrest by Mitochondrial ATP-Sensitive Potassium Channels. Biomed Res Int 2016;2016:1253842.

[2]Coetzee WA. Multiplicity of effectors of the cardioprotective agent, diazoxide. Pharmacol Ther. 2013 Nov;140(2):167-75.

[3]Coetzee WA. Multiplicity of effectors of the cardioprotective agent, diazoxide. Pharmacol Ther. 2013;140(2):167-175

[4]Virgili N, Mancera P, Wappenhans B, et al. K(ATP) channel opener diazoxide prevents neurodegeneration: a new mechanism of action via antioxidative pathway activation [published correction appears in PLoS One. 2013 Sep 19;8(9):null]. PLoS One. 2013;8(9):e75189. Published 2013 Sep 11

[5]Wu H, Wang P, Li Y, Wu M, Lin J, Huang Z. Diazoxide Attenuates Postresuscitation Brain Injury in a Rat Model of Asphyxial Cardiac Arrest by Opening Mitochondrial ATP-Sensitive Potassium Channels. Biomed Res Int. 2016;2016:1253842