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Fomepizole

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Rating icon 很棒

纯度: 99.94%

货号 T0765Cas号 7554-65-6

别名 甲吡唑, Antizol-Vet, Antizol, 4-甲基吡唑, 4-Methylpyrazole

Fomepizole (4-Methylpyrazole) 是细胞色素 P450 (CYP2E1) 抑制剂。它是乙醇脱氢酶 (alcohol dehydrogenase) 竞争性抑制剂。它能够阻断甲醇和乙二醇进一步转化为有毒代谢产物。它具有成为乙二醇或甲醇中毒的解毒剂的潜力。

Fomepizole
其他形式的 “Fomepizole”:

Fomepizole

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Rating icon 很棒

纯度: 99.94%

货号 T0765 别名 甲吡唑, Antizol-Vet, Antizol, 4-甲基吡唑, 4-MethylpyrazoleCas号 7554-65-6

Fomepizole (4-Methylpyrazole) 是细胞色素 P450 (CYP2E1) 抑制剂。它是乙醇脱氢酶 (alcohol dehydrogenase) 竞争性抑制剂。它能够阻断甲醇和乙二醇进一步转化为有毒代谢产物。它具有成为乙二醇或甲醇中毒的解毒剂的潜力。

规格价格库存数量
100 mg
¥ 167
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500 mg
¥ 350
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1 g
¥ 493
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1 mL x 10 mM (in DMSO)
¥ 418
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产品介绍


Fomepizole AI Summary
Fomepizole has inhibitory activity against horse liver alcohol dehydrogenase with a Ki value of 141.25 nM and a Kd value of 13.0 nM. Its partition coefficient (logP) is 0.96. This compound exhibits bioactivity in multiple assays, including inhibition of GCN5L2, Histone Lysine Methyltransferase G9a, T. brucei phosphofructokinase, and Marburg Virus entry, showing nanomolar potency in these bioassays. However, it has minimal hepatic side effects, with HepSE scores for various liver-related conditions all reporting 0.0, indicating no bioactivity in causing liver injury or dysfunction according to the DILIps training set data. Despite showing some antiviral activity against SARS-CoV-2 in VERO-6 cells with an IC50 value greater than 20,000.0 nM, it demonstrates low bioactivity in inhibiting cell viability of Vero E6 cells infected with SARS-CoV-2 and moderate activity in HRCE cells against the USA-WA1/2020 strain. The compound also shows 11.82% inhibition of SARS-CoV-2 3CL-Pro protease at a 20 µM concentration. Moreover, it impacts various biomarkers such as ALT, AST, BUN, and others, suggesting potential hepatotoxic, nephrotoxic, and hematotoxic effects. Despite binding affinities towards several receptors like Grin1, ADRB2, CHRNA4, OPRK1, and HTR2C with AC50 values greater than 10,000 nM, it has not shown significant inhibition or agonist activity in most assays conducted..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Fomepizole (4-Methylpyrazole) is used as an antidote in confirmed or suspected methanol or ethylene glycol poisoning. Fomepizole(4-Methylpyrazole) is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.
别名甲吡唑, Antizol-Vet, Antizol, 4-甲基吡唑, 4-Methylpyrazole
化学信息
分子量82.1
分子式C4H6N2
CAS No.7554-65-6
SmilesCC1=CNN=C1
密度1.015 g/cm3. Temperature:20 °C.
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
H2O: 100 mg/mL (1218.03 mM), Sonication is recommended.
DMSO: 250 mg/mL (3045.07 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (24.36 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
H2O/DMSO
1mg5mg10mg50mg
1 mM12.1803 mL60.9013 mL121.8027 mL609.0134 mL
5 mM2.4361 mL12.1803 mL24.3605 mL121.8027 mL
10 mM1.2180 mL6.0901 mL12.1803 mL60.9013 mL
20 mM0.6090 mL3.0451 mL6.0901 mL30.4507 mL
50 mM0.2436 mL1.2180 mL2.4361 mL12.1803 mL
100 mM0.1218 mL0.6090 mL1.2180 mL6.0901 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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