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Prothionamide

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纯度: 99.34%

货号 T1161Cas号 14222-60-7

别名 丙硫异烟胺, Protionamide, 1321-TH

Prothionamide (1321-TH) 是一种具有抗结核活性的硫代酰胺衍生物。它可作用于结核病和麻风病。

Prothionamide

Prothionamide

一键复制产品信息
Rating icon 很棒

纯度: 99.34%

货号 T1161 别名 丙硫异烟胺, Protionamide, 1321-THCas号 14222-60-7

Prothionamide (1321-TH) 是一种具有抗结核活性的硫代酰胺衍生物。它可作用于结核病和麻风病。

规格价格库存数量
200 mg
¥ 99
现货
1 mL x 10 mM (in DMSO)
¥ 99
现货
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产品介绍


Prothionamide AI Summary
Prothionamide is a multifaceted bioactive molecule displaying various pharmacological effects. It shows strong inhibitory activity against several targets such as the malarial parasite plastid (potency of 82.8 nM), Mycobacterium tuberculosis (IC50 of 6610.0 nM in 7H9 media and enhanced activity with MIC50 values reduced up to 500.0 nM in the presence of specific inhibitors), and the enzyme tyrosyl-DNA phosphodiesterase 1 (TDP1) with a potency of 29092.9 nM. Additionally, it serves as an agonist for the Thyroid Stimulating Hormone Receptor with a potency of 31622.8 nM and an activator of Cytochrome P450 3A4 at 39810.7 nM. Clinically significant liver toxicity has been observed, indicated by elevated serum ALT and AST levels. The compound shows moderate hepatotoxicity with a rating of 8.0 and a highest observed frequency of 13.0% during trials. Acute liver toxicity was noted with a hepatic rating of 7.0 and a 2.5% highest frequency rate. Cytolytic liver toxicity is reported with a rating of 4.0, while no significant cholestatic liver toxicity is observed (rating of 0.0). Prothionamide also exhibits antiviral properties, specifically against SARS-CoV-2, inhibiting viral cytotoxicity in Vero E6 cells and Caco-2 cells at various concentrations. However, the efficacy varies, with inhibition scores ranging from 0.1% to over 30%, and an IC50 value exceeding 19952.62 nM, indicating moderate antiviral potency. Furthermore, it shows potential inhibitory activity against the SARS-CoV-2 3CL-Pro protease, though with an inhibition rate of -2.174% at 20µM suggesting a need for optimization. The compound demonstrates notable antimycobacterial activity against both standard and GFP expressing strains of Mycobacterium tuberculosis, especially in combination with EthR inhibitors, and has a minimum inhibitory concentration of 0.3 ug/mL for a strain harboring the inhA gene. Additionally, as a tyrosinase inhibitor, Prothionamide inhibits both mushroom tyrosinase and tyrosinase in mouse B16F10 cells, showing non-competitive inhibition and binding affinity. It also shows cytotoxicity against these cells at specific concentrations. Overall, Prothionamide is versatile with applications ranging from antimicrobial and anti-parasitic to antiviral activities, with significant liver safety considerations that must be carefully managed in clinical settings..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Prothionamide (1321-TH)is a thioamide derivative with antitubercular activity.
别名丙硫异烟胺, Protionamide, 1321-TH
化学信息
分子量180.27
分子式C9H12N2S
CAS No.14222-60-7
SmilesCCCC1=NC=CC(=C1)C(N)=S
密度1.1015 g/cm3 (Estimated)
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
Ethanol: 7 mg/mL (38.83 mM), Sonication is recommended.
DMSO: 55 mg/mL (305.1 mM), Sonication is recommended.
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 (11.09 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
Ethanol/DMSO
1mg5mg10mg50mg
1 mM5.5472 mL27.7362 mL55.4723 mL277.3617 mL
5 mM1.1094 mL5.5472 mL11.0945 mL55.4723 mL
10 mM0.5547 mL2.7736 mL5.5472 mL27.7362 mL
20 mM0.2774 mL1.3868 mL2.7736 mL13.8681 mL
DMSO
1mg5mg10mg50mg
50 mM0.1109 mL0.5547 mL1.1094 mL5.5472 mL
100 mM0.0555 mL0.2774 mL0.5547 mL2.7736 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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