Ethoxzolamide (Redupresin)
(Synonyms: 乙氧苯噻唑胺,Redupresin; L-643786; PNU-4191) 目录号 : GC31710
Ethoxzolamide (Redupresin) 是一种碳酸酐酶抑制剂，Ki 为 1 nM。
Cas No.:452-35-7
Sample solution is provided at 25 µL, 10mM.
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Ethoxzolamide is a carbonic anhydrase inhibitor with Ki of 1 nM.
Ethoxzolamide (ETZ) treatment causes >90% inhibition of reporter GFP fluorescence in infected macrophages. Moreover, in a 9-day macrophage survival assay, Ethoxzolamide (ETZ) treatment significantly inhibits the ability of M. tuberculosis to grow intracellularly[2].
It is discovered that the lipid-soluble ethoxzolamide is converted in vivo to a water-soluble metabolite, while retaining high activity againstt the enzyme. At the minimal dose for maximal effect (4 mg/kg i.v. at 45 min) the IOP lowering is 4.2 mmHg, the concentration in anterior uvea is 2.5 pmol/kg, and the fractional inhibition of the enzyme (i) is 0.9995. The effect declines rapidly, attributable to the very short half-life of drug in plasma, leading to depletion of free drug in the anterior uvea and other tissues[1]. Ethoxzolamide (ETZ) strongly downregulates GFP reporter fluorescence in mouse lungs, with 3-fold inhibition of GFP signal compare to that in the mock-treating control. There is a significant reduction of bacterial survival in the lungs of ETZ-treating mice compare to the mock-treating control[2].
[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.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [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. | |
| Cas No. | 452-35-7 | SDF | |
| 别名 | 乙氧苯噻唑胺,Redupresin; L-643786; PNU-4191 | ||
| Canonical SMILES | O=S(C1=NC2=CC=C(OCC)C=C2S1)(N)=O | ||
| 分子式 | C9H10N2O3S2 | 分子量 | 258.32 |
| 溶解度 | DMSO : 150 mg/mL (580.68 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8712 mL | 19.3558 mL | 38.7117 mL |
| 5 mM | 0.7742 mL | 3.8712 mL | 7.7423 mL |
| 10 mM | 0.3871 mL | 1.9356 mL | 3.8712 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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