| CAS |
No.59-66-5 |
| 中文名称 |
乙酰唑胺(10mM in DMSO,无菌） |
| 英文名称 |
Acetazolamide(10mM in DMSO，Sterile） |
| 分子式 |
C4H6N4O3S2 |
| 分子量 |
222.25 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
Carbonic Anhydrase |
| 通路 |
Metabolic Enzyme&Protease |
| 背景说明 |
是一种碳酸酐酶抑制剂。 |
| 生物活性 |
Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX. Acetazolamide has diuretic， antihypertensive and anti-gonococcal activities.[1-6] |
| In Vitro |
Acetazolamide also inhibits hCA II with an IC50 of 130 nM[1]. Acetazolamide (Ace) is a small heteroaromatic sulfonamide that binds to various carbonic anhydrases with high affinity， acting as a carbonic anhydrase (CA) inhibitor[2].Compared with the control group， the high Acetazolamide concentration (AceH， 50 nM)， Cisplatin (Cis; 1 μg/mL) and Cis combined with the low Acetazolamide concentration (AceL， 10 nM) treatments significantly reduces viability of Hep-2 cells[2].Treatment with the Acetazolamide/Cis combination significantly increases the expression levels of P53， as both AceL+Cis and AceH+Cis treatments result in significantly increased P53 protein expression levels compared with the control group. The Ace/Cis combination treatment significantly reduces the bcl-2/bax expression ratio， and increases the expression of caspase-3 protein， compared with the control group. AceL， AceH， Cis and AceL+Cis treatments significantly reduce the bcl-2/bax ratio compared with the control group[2].
Combined Ace and Cis treatment effectively promotes apoptosis in Hep-2 cells[2].
Combined treatment with Ace/Cis markedly decreases the expression of AQP1 mRNA in Hep-2 cells. Both AceH and AceL+Cis treatments decrease the expression of aquaporin-1 (AQP1) mRNA in Hep-2 cells compared with the control group[2]. |
| In Vivo |
Acetazolamide (40 mg/kg) significantly potentiates the inhibitory effect of MS-275 on tumorigenesis in neuroblastoma (NB) SH-SY5Y xenografts[3].
Acetazolamide (40 mg/kg) and/or MS-275 treatment reduce expression of HIF1-α and CAIX in NB SH-SY5Y xenograft[3].
Acetazolamide (40 mg/kg)， MS-275 and Acetazolamide+MS-275 reduce expression of mitotic and proliferative markers in NB SH-SY5Y xenografts[3].
Acetazolamide (50 mg/kg; PO， for 3 days) significantly reduces the gonococcal load in the vagina of infected mice by 90%[6]. |
| 细胞实验 |
Cell Viability Assay[2]
Cell line: Hep-2 cells and HUVECs;Concentration: 10 nM and 50 nM;Incubation time: 48 h;Assay: The cell viability of Hep-2 cells and HUVECs is measured by MTT assay. Hep-2 cells and HUVECs in logarithmic growth phase are plated in 96-well plates. Following 48 h of drug treatment as indicated， 200 μL MTT (5 mg/mL) is added to each well. Cells are incubated with the MTT solution at 37°C for 4 h. Then， 150 μL DMSO is added for 5 min. The optical density (OD) values are measured at 490 nm with a Versamax Microplate reader. |
| 动物实验 |
In vivo studies[3]
Animal model: 4-6 weeks-old female NOD/SCID mice;Dosage: 40 mg/kg， intraperitoneal injection， every day for 2 weeks;Administration: Mice are randomized into four groups (5 mice per group). The control and treatment groups receive intraperitoneal injections of vehicle (PBS) or Acetazolamide (40 mg/kg)， MS-275 (20 mg/kg) or the combination， respectively， every day for 2 weeks. Experiments are terminated when tumor sizes exceed 2 cm3 in volume or animals show signs of morbidity. Tumor diameters are measured on a daily basis until termination. |
| 数据来源文献 |
[1]. Hou Z， et al. Dual-tail approach to discovery of novel carbonic anhydrase IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site. Eur J Med Chem. 2017 May 26;132:1-10.
[2]. Bayat Mokhtari R， et al. Acetazolamide potentiates the anti-tumor potential of HDACi， MS-275， in neuroblastoma. BMC Cancer. 2017 Feb 24;17(1):156.
[3]. Gao H， et al. Combined treatment with acetazolamide and cisplatin enhances chemosensitivity in laryngeal carcinoma Hep-2 cells. Oncol Lett. 2018 Jun;15(6):9299-9306.
[4]. Kassamali R， et al. Acetazolamide: a forgotten diuretic agent. Cardiol Rev. 2011 Nov-Dec;19(6):276-8.
[5]. Jabeen E， et al. Interaction of antihypertensive acetazolamide with nonsteroidal anti-inflammatory drugs. J Photochem Photobiol B. 2013 Aug 5;125:155-63.
[6]. Abutaleb NS， et al. In vivo efficacy of acetazolamide in a mouse model of Neisseria gonorrhoeae infection. Microb Pathog. 2022 Mar;164:105454. |
| 规格 |
0.1ml 0.3ml 0.5ml 1ml 1.5ml |
| 单位 |
瓶 |
中文
英语
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