1. Membrane Transporter/Ion Channel Autophagy
  2. Potassium Channel Autophagy
  3. Diazoxide

Diazoxide  (Synonyms: 二氮嗪; Sch-6783; SRG-95213)

目录号: HY-B1140 纯度: 99.99%
COA 产品使用指南

Diazoxide (Sch-6783) 是一种 ATP 敏感性的钾离子通道 (potassium channel) 激活剂,有潜力用于高胰岛素血症的研究。

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Diazoxide Chemical Structure

Diazoxide Chemical Structure

CAS No. : 364-98-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
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100 mg ¥500
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200 mg   询价  
500 mg   询价  

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Customer Review

Other Forms of Diazoxide:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
23.5 μM
Compound: 3
Activation of human recombinant SUR1/Kir6.2 channel expressed in HEK293 cells assessed as increase in ionic current by whole cell patch clamp assay
Activation of human recombinant SUR1/Kir6.2 channel expressed in HEK293 cells assessed as increase in ionic current by whole cell patch clamp assay
[PMID: 19919106]
HEK293 IC50
33 μM
Compound: Diazoxide
Potency by glucose stimulated insulin release from HEK 293 cells
Potency by glucose stimulated insulin release from HEK 293 cells
[PMID: 15501029]
体外研究
(In Vitro)

Diazoxide (Sch-6783) 具有多种生理作用,包括降低血压和纠正低血糖症。Diazoxide 具有强大的抗心肌缺血保护特性[1]
Diazoxide (Sch-6783) 可以保护 NSC-34 神经元免受神经退行性损伤的主要来源。Diazoxide 增加 NSC-34 运动神经元中的 Nrf2 核转位并防止内源性氧化损伤[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Diazoxide (Sch-6783) 可减轻复苏后脑损伤,保护线粒体功能,抑制脑细胞凋亡,并通过打开 mitoKATP 通道激活 PKC 通路[3]
Diazoxide (Sch-6783) 处理在野生型小鼠中降低眼压 (IOP) 21.5±3.2%,绝对 IOP 降低 3.9 ± 0.6 mm Hg[4]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

230.67

Formula

C8H7ClN2O2S

CAS 号
性状

固体

颜色

White to gray

中文名称

二氮嗪;氯甲苯噻嗪;氯苯甲噻二嗪

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 35 mg/mL (151.73 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.3352 mL 21.6760 mL 43.3520 mL
5 mM 0.8670 mL 4.3352 mL 8.6704 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (9.02 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (9.02 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.99%

参考文献
Cell Assay
[2]

Diazoxide is dissolved in DMSO to prepare 50 mM stock solution. NSC-34 cells are allowed to differentiate for 8 weeks under reduced serum conditions and then seeded in 24-well plates. Glutamate is dissolved in culture medium and added to cultures at concentration of 10 μM for 24 h. Cell treatment with 100 µM diazoxide starts 2 h before glutamate exposure. Cell viability is measured by the MTT assay[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3][4]

Rats: Adult male Sprague-Dawley rats with induced cerebral ischemia (n=10 per group) receive an intraperitoneal injection of 0.1% DMSO (1 mL; vehicle group), diazoxide (10 mg/kg; DZ group), or diazoxide (10 mg/kg) plus 5-hydroxydecanoate (5 mg/kg; DZ + 5-HD group) 30 min after CPR. The control group (sham group, n=5) undergoes sham operation, without cardiac arrest. Mitochondrial respiratory control rate (RCR) is determined. Brain cell apoptosis is assessed using TUNEL staining. Expression of Bcl-2, Bax, and protein kinase C epsilon (PKCε) in the cerebral cortex is determined by Western blotting and immunohistochemistry[3].

Mouse: Diazoxide is prepared by diluting a 100 mM stock solution in 10% polyethoxylated castor oil in PBS. In C57BL/6 wild-type and Kir6.2(−/−) mice, a 5 μL drop of 5 mM diazoxide is topically administered to one eye of each mouse while the fellow control eye received vehicle (DMSO and 10% polyethoxylated castor oil in the same proportion as the treated eye). IOP is measured daily at 1 hour, 4 hours, and 23 hours following treatment. Treatment with diazoxide and vehicle is continued daily for 14 consecutive days[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3352 mL 21.6760 mL 43.3520 mL 108.3799 mL
5 mM 0.8670 mL 4.3352 mL 8.6704 mL 21.6760 mL
10 mM 0.4335 mL 2.1676 mL 4.3352 mL 10.8380 mL
15 mM 0.2890 mL 1.4451 mL 2.8901 mL 7.2253 mL
20 mM 0.2168 mL 1.0838 mL 2.1676 mL 5.4190 mL
25 mM 0.1734 mL 0.8670 mL 1.7341 mL 4.3352 mL
30 mM 0.1445 mL 0.7225 mL 1.4451 mL 3.6127 mL
40 mM 0.1084 mL 0.5419 mL 1.0838 mL 2.7095 mL
50 mM 0.0867 mL 0.4335 mL 0.8670 mL 2.1676 mL
60 mM 0.0723 mL 0.3613 mL 0.7225 mL 1.8063 mL
80 mM 0.0542 mL 0.2709 mL 0.5419 mL 1.3547 mL
100 mM 0.0434 mL 0.2168 mL 0.4335 mL 1.0838 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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