二氮嗪 T0126

Product Introduction
Bioactivity


英文名: Diazoxide

描述: Diazoxide (Proglycem) 是一种 ATP 敏感性的钾离子通道激活剂，是一种苯并噻二嗪衍生物，是一种用于高血压急症的外周血管扩张剂。

细胞实验: The phagocytic ability of microglia is determined by the uptake of 2-μm red fluorescent microspheres by BV-2 cells. Cells are treated with diazoxide 100 μM and activated with LPS/IFN-γ and then incubated with microspheres at a concentration of 0.01% for 30 min in the dark at 37°C and 5% CO2. Cells are rinsed twice in PBS solution, pelleted at 1,000 g for 5 min and resuspended in 300 μL PBS. Cells are kept on ice and analyzed by flow cytometry.(Only for Reference)

体外活性: Diazoxide 可抑制小胶质细胞的炎症活动。Diazoxide 处理可部分抑制 LPS/IFN-γ 在小胶质细胞中诱导的炎症模式，诱导 NO 生成的减少可能是由于检测到 iNOS 表达的减少。Diazoxide 对小胶质细胞的吞噬作用没有影响[1]。

体内活性: Diazoxide 有利于改善认知任务、减轻焦虑、减少淀粉样蛋白-β寡聚体的积累和 tau 蛋白的过度磷酸化。Diazoxide 还可以通过降低神经元的兴奋性和激活 N-甲基-D-天冬氨酸（NMDA）受体，或增加α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体的电流，在激活 K+ 通道之外发挥神经保护作用。经Diazoxide 处理的动物在出现首批临床症状几天后（即疾病的急性炎症期），疾病的严重程度会有所减轻。在EAE小鼠的效应期，每天口服Diazoxide 可减轻临床症状的严重程度，且无任何明显的不良反应。二氮氧化物可减少脱髓鞘和轴突丢失，减轻组织损伤，抑制小胶质细胞/巨噬细胞和星形胶质细胞的活化，保护神经元的完整性。对浸润脊髓的 B 淋巴细胞和 T 淋巴细胞的数量没有影响[1]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 43 mg/mL (186.4 mM)


关键字: Sch6783 | Autophagy | Potassium Channel | SRG 95213 | inhibit | Inhibitor | Diazoxide | SRG95213 | Sch 6783 | KcsA

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相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Approved Drug Library | Mitochondria-Targeted Compound Library | Drug-induced Liver Injury (DILI) Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途