中文名称: | 依索唑胺 | ||||
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英文名称: | Ethoxzolamide | ||||
别名: | 依索唑胺;乙氧苯噻唑胺;6-乙氧基-2-苯并噻唑磺酰胺;1-硝基金刚烷;乙氧苯噻唑胺 USP标准品 Redupresin; L-643786; PNU-4191;6-Ethoxyzolamide;6-Ethoxy-2-benzothiazolesulfonamide | ||||
CAS No: | 452-35-7 | 分子式: | C9H10N2O3S2 | 分子量: | 258.32 |
CAS No: | 452-35-7 | ||||
分子式: | C9H10N2O3S2 | ||||
分子量: | 258.32 | ||||
MDL: | MFCD00057089 | EINEC: | 207-199-5 | ||
EINEC: | 207-199-5 |
基本信息
产品编号: |
E10296 |
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产品名称: |
Ethoxzolamide |
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CAS: |
452-35-7 |
储存条件 |
粉末 |
室温 |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
258.32 |
-20℃ |
一个月 |
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化学名: |
6-Ethoxy-2-benzothiazolesulfonamide |
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Solubility (25°C): |
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体外:
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DMSO |
≥100mg/mL(387.12mM) |
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Ethanol |
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Water |
<0.1mg/mL(insoluble) |
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体内(现配现用): |
1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.08mg/mL(8.05mM);Clear solution |
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此⽅案可获得≥2.08mg/mL(8.05mM,饱和度未知)的澄清溶液。以1mL⼯作液为例,取100μL20.8mg/mL的澄清DMSO储备液加到400μL PEG300中,混合均匀;向上述体系中加⼊50μL Tween-80,混合均匀;然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 |
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2.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility:≥2.08mg/mL(8.05mM);Clear solution |
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此⽅案可获得≥2.08mg/mL(8.05mM,饱和度未知)的澄清溶液。以1mL⼯作液为例,取100μL20.8mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中,混合均匀。 |
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3.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility:≥2.08mg/mL(8.05mM);Clear solution |
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此⽅案可获得≥2.08mg/mL(8.05mM,饱和度未知)的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例,取100μL20.8mg/mL的澄清DMSO储备液加到900μL⽟⽶油中,混合均匀。 |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
3.8712mL |
19.3558mL |
38.7117mL |
5mM |
0.7742mL |
3.8712mL |
7.7423mL |
10mM |
0.3871mL |
1.9356mL |
3.8712mL |
生物活性
产品描述 |
是 carbonic anhydrase 的抑制剂,其 Ki 值为 1nM。 |
靶点 |
Ki: 1nM (carbonic anhydrase) |
体外研究 |
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 |
体内研究 |
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. 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 |
推荐实验方法(仅供参考)
Cell Assay |
BMDMs are treated with 80μM 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 100μM Ethoxzolamide (ETZ) or an equal volume of DMSO for 9 days |
Animal Administration |
Rats (male, 300–325g) 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 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )