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Sulfisoxazole

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纯度: 99.98%

货号 T0750Cas号 127-69-5

别名 磺胺异恶唑, 磺胺二甲异唑, Sulfafurazole, NU-445

Sulfisoxazole (Sulfafurazole) 是一种内皮素受体拮抗剂,是磺胺类抗生素。它靶向内皮素受体 A,抑制乳腺癌外显子释放。

Sulfisoxazole
其他形式的 “Sulfisoxazole”:

Sulfisoxazole

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Rating icon 很棒

纯度: 99.98%

货号 T0750 别名 磺胺异恶唑, 磺胺二甲异唑, Sulfafurazole, NU-445Cas号 127-69-5

Sulfisoxazole (Sulfafurazole) 是一种内皮素受体拮抗剂,是磺胺类抗生素。它靶向内皮素受体 A,抑制乳腺癌外显子释放。

规格价格库存数量
50 mg
¥ 178
现货
100 mg
¥ 247
现货
200 mg
¥ 329
现货
500 mg
¥ 496
现货
1 g
¥ 723
现货
1 mL x 10 mM (in DMSO)
¥ 272
现货
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产品介绍


Sulfisoxazole AI Summary
Sulfisoxazole exhibits multifaceted bioactivity and pharmacokinetic properties, making it a significant compound for research. It shows potent inhibition of the Endothelin A receptor with an IC50 ranging from 780.0 nM to 9000.0 nM, indicating its strong interaction with this receptor in various systems, including rat aortic smooth muscle cells and human cells. Its binding affinity is much lower for the Endothelin B receptor, with an IC50 of 24000.0 nM. Pharmacokinetically, Sulfisoxazole has high oral bioavailability (>80%) and significant plasma protein binding in humans (91.28%), dogs (86.59%), and rats (98.47%). It demonstrates moderate clearance rates and distribution, with a total clearance of 0.3 mL.min-1.kg-1 and a volume of distribution at steady state of 0.17 L.kg-1. Its physicochemical properties include a logD6.5 value of -0.5 and a pKa of 5.0. Additionally, Sulfisoxazole exhibits bioactivity as an inhibitor of the Menin-MLL interaction, Thyroid Stimulating Hormone Receptor, Cytochrome P450 2C19, and various other targets. It shows antimicrobial activity against bacteria like Escherichia coli and Staphylococcus epidermidis, and antifungal activity against Aspergillus fumigatus, with MIC values indicating broad-spectrum bioactivity. Despite some liver toxicity and moderate liver clearance rates, it demonstrates low intrinsic clearance rates in rat hepatocytes and human liver microsomes, suggesting slow metabolism. Sulfisoxazole also shows antiviral activity against SARS-CoV-2, albeit with limited effectiveness according to various assays, including cytotoxicity and 3CL-Pro protease inhibition. Furthermore, it has been identified to inhibit the Bile Salt Export Pump (BSEP), though at high IC50 values (>135000.0 nM), indicating weak inhibition. Overall, Sulfisoxazole’s broad bioactivity profile, significant pharmacokinetic properties, and multi-target inhibition suggest its potential application in various therapeutic areas, albeit with caution due to its hepatotoxicity and moderate liver toxicity..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Sulfisoxazole (Sulfafurazole) is a short-acting sulfonamide antibacterial with activity against a wide range of gram-negative and gram-positive organisms.Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A.
靶点活性
ETB:22 microM, ETA:0.60 microM
别名磺胺异恶唑, 磺胺二甲异唑, Sulfafurazole, NU-445
化学信息
分子量267.30
分子式C11H13N3O3S
CAS No.127-69-5
SmilesCC1=NOC(NS(=O)(=O)C2=CC=C(N)C=C2)=C1C
密度1.411g/cm3
颜色White
物理性状Solid
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 250 mg/mL (935.28 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.48 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM3.7411 mL18.7056 mL37.4111 mL187.0557 mL
5 mM0.7482 mL3.7411 mL7.4822 mL37.4111 mL
10 mM0.3741 mL1.8706 mL3.7411 mL18.7056 mL
20 mM0.1871 mL0.9353 mL1.8706 mL9.3528 mL
50 mM0.0748 mL0.3741 mL0.7482 mL3.7411 mL
100 mM0.0374 mL0.1871 mL0.3741 mL1.8706 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments 比如您的给药剂量是10 mg/kg,每只动物体重20g,给药体积100 μLTargetMol | Animal experiments 一共给药动物10只,您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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