| CAS |
No.452-35-7 |
| 中文名称 |
依索唑胺 |
| 英文名称 |
Ethoxzolamide |
| 分子式 |
C9H10N2O3S2 |
| 分子量 |
258.32 |
| 溶解性 |
Soluble in DMSO ≥10mg/mL |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 靶点 |
Carbonic Anhydrase |
| 通路 |
Metabolic Enzyme&Protease |
| 背景说明 |
Ethoxzolamide 是 carbonic anhydrase 的抑制剂。 |
| 生物活性 |
Ethoxzolamide is a carbonic anhydrase inhibitor with Ki of 1 nM.[1-3] |
| IC50 |
Ki: 1 nM (carbonic anhydrase)[1] |
| In Vitro |
Ethoxzolamide (ETZ) 处理导致受感染的巨噬细胞中的报告 GFP 荧光抑制 >90%。此外，在为期 9 天的巨噬细胞存活测定中，Ethoxzolamide (ETZ) 处理显著抑制了 M. tuberculosis 在细胞内生长[2]。 |
| In Vivo |
发现脂溶性乙氧唑胺在体内转化为水溶性代谢物，同时保持对酶的高活性。在达到最大效果的最小剂量 (4 mg/kg iv，45 分钟) 下，IOP 降低为 4.2 mmHg，前葡萄膜中的浓度为 2.5 pmol/kg，酶 (i) 的抑制分数为 0.9995。由于药物在血浆中的半衰期非常短，导致前葡萄膜和其他组织中的游离药物耗尽，因此作用迅速下降[1]。Ethoxzolamide (ETZ) 强烈下调小鼠肺部的 GFP 报告基因荧光，与模拟处理对照相比，GFP 信号抑制 3 倍。与模拟处理对照组相比，接受 ETZ 处理的小鼠肺部细菌存活率显著降低[2]。 |
| 细胞实验 |
BMDMs are treated with 80 μM Ethoxzolamide (ETZ) or an equivalent volume of DMSO every 2 days for 9 days total. At days 3， 6， and 9， intracellular bacteria are quantified by lysing macrophage monolayers and performing serial dilution plating of lysates on 7H10 agar. For fluorescence microscopy experiments， macrophages are seeded on glass coverslips before infection with M. tuberculosis CDC1551. Samples are treated every 2 days with 100 μM Ethoxzolamide (ETZ) or an equal volume of DMSO for 9 days[2]. |
| 动物实验 |
Rats (male， 300–325 g) are randomly selected into 2 groups (n=6 each group) and Ethoxzolamide (EZ) is administered at a dose of 0.18 mg/kg (in PEG 300: ethanol， 1:1) via i.v. injection through the tail vein. Blood samples (about 50-100 μL) are collected in heparinizing tubes at 0， 15， 30， 60， 120， 180， 240， 360， 540， and 1440 min post-injection， via tail snip with isoflurane as anesthetic. Plasma samples are prepared and stored at -80 °C until analysis. To study the distribution in brain， rats in group 1 are scarified at 6 hours and rats in group 2 are scarified at 24 hours to collect the brain tissues. Those blood samples from group 2 are analyzed to generated PK profile[3]. |
| 数据来源文献 |
[1]. Maren TH， et al. Relations among IOP reduction， ocular disposition and pharmacology of the carbonic anhydrase inhibitor ethoxzolamide. Exp Eye Res. 1992 Jul;55(1):73-9.
[2]. Benjamin K. Johnson， et al. The Carbonic Anhydrase Inhibitor Ethoxzolamide Inhibits theMycobacterium tuberculosis PhoPR Regulon and Esx-1 Secretion and Attenuates Virulence. Antimicrob Agents Chemother. 2015 Aug; 59(8): 4436–4445.
[3]. Song Gao， et al. Development and validation of an UPLC-MS/MS method for the quantification of ethoxzolamide in plasma and bioequivalent buffers: Applications to absorption， brain distribution， and pharmacokinetic studies. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Apr 1; 0: 54–59. |
| 规格 |
100mg |
| 单位 |
瓶 |
中文
英语
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