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Thiamphenicol

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纯度: 99.8%

货号 T1550Cas号 15318-45-3

别名 甲砜霉素, Thiophenicol, Dextrosulphenidol

Thiamphenicol (Dextrosulphenidol) 是 Chloramphenicol 的甲基磺酰基衍生物,是一种广谱抗菌类抗生素。它与 50S 核糖体亚基结合,抑制蛋白质合成并具有抑菌作用 ,特别针对革兰氏阴性,革兰氏阳性需氧和厌氧菌。

Thiamphenicol

Thiamphenicol

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Rating icon 很棒

纯度: 99.8%

货号 T1550 别名 甲砜霉素, Thiophenicol, DextrosulphenidolCas号 15318-45-3

Thiamphenicol (Dextrosulphenidol) 是 Chloramphenicol 的甲基磺酰基衍生物,是一种广谱抗菌类抗生素。它与 50S 核糖体亚基结合,抑制蛋白质合成并具有抑菌作用 ,特别针对革兰氏阴性,革兰氏阳性需氧和厌氧菌。

规格价格库存数量
50 mg
¥ 178
现货
100 mg
¥ 247
现货
500 mg
¥ 413
现货
1 g
¥ 579
现货
1 mL x 10 mM (in DMSO)
¥ 148
现货
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产品介绍


Thiamphenicol AI Summary
Thiamphenicol exhibits a range of bioactivities and physicochemical properties. It has been tested for inhibition of the puromycin reaction, demonstrating an inhibition constant (Ki) of 400.0 nM. The compound has a moderate hydrophobic profile with a low partition coefficient (logP) and a logD7.4 of -0.27, indicating a preference for the aqueous layer over the organic layer at physiological pH. It shows cytotoxic activity against various strains of Streptococcus and inhibition of Streptokinase Promoter Activity, with EC50 values ranging from 740.0 nM to 4552.0 nM. Additionally, it inhibits the PhoP region in Salmonella Typhimurium with IC50 values between 18030.0 nM and 86160.0 nM. Thiamphenicol demonstrates inhibitory effects on several targets, including human tyrosyl-DNA phosphodiesterase 1, malaria parasite plastid, HP1-beta Chromodomain interactions, and Plasmodium falciparum proliferation, with potency values ranging from 2269.5 nM to 89125.1 nM. It has anti-SARS-CoV-2 activity, inhibiting the SARS-CoV-2 3CL-Pro protease by 16.32% at 20µM and reducing cytotoxicity in Caco-2 and VERO-6 cells at various concentrations. The compound exhibits moderate hepatotoxicity, with evidence of acute liver toxicity, and affects several liver function parameters (ALT, AST, ALP, and bilirubin) as well as kidney function markers and blood chemistry parameters. It shows inhibitory activity towards human HDAC6 enzyme, with an inhibition rate of 10.91% using a commercial peptide substrate. In transporter assays, Thiamphenicol inhibits multiple transport proteins such as BSEP, MRP2, MRP3, and MRP4 with relatively low potency (IC50 values >133000.0 nM). It also affects sodium fluorescein uptake in OATP1B3- and OATP1B1-transfected cells, with inhibitions over 100%. Overall, Thiamphenicol has diverse pharmacological effects on multiple biological pathways and targets, suggesting its potential utility in various therapeutic areas, albeit with a cautionary note regarding its hepatotoxic and nephrotoxic potential..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Thiamphenicol (Dextrosulphenidol) is a methylsulfonyl analog of chloramphenicol. It is an antibiotic and immunosuppressive agent.
别名甲砜霉素, Thiophenicol, Dextrosulphenidol
化学信息
分子量356.22
分子式C12H15Cl2NO5S
CAS No.15318-45-3
Smiles[C@@H]([C@H](NC(C(Cl)Cl)=O)CO)(O)C1=CC=C(S(C)(=O)=O)C=C1
密度1.3281 g/cm3 (Estimated)
储存&溶解度
存储keep away from moisture,keep away from direct sunlight | 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: 55 mg/mL (154.4 mM), Sonication is recommended.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.61 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 mM2.8073 mL14.0363 mL28.0725 mL140.3627 mL
5 mM0.5615 mL2.8073 mL5.6145 mL28.0725 mL
10 mM0.2807 mL1.4036 mL2.8073 mL14.0363 mL
20 mM0.1404 mL0.7018 mL1.4036 mL7.0181 mL
50 mM0.0561 mL0.2807 mL0.5615 mL2.8073 mL
100 mM0.0281 mL0.1404 mL0.2807 mL1.4036 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:
比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL, 一共给药动物10只,您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O, 那么您的工作液浓度为2 mg/mL
母液配置方法:2 mg 药物溶于 100 μL DMSO ( 母液浓度为 20 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:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 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: DMSOPEG300PEG400Tween 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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