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Isoxicam

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纯度: 99.02%

货号 T0285Cas号 34552-84-6

别名 伊索昔康, Maxicam, Isoxicamum, Isoxicamo

Isoxicam (Isoxicamum) 是可口服的非甾体抗炎剂,可通过抑制环氧合酶 1 和 2 来阻断前列腺素的合成,可用于关节炎的研究。

Isoxicam
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Isoxicam

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Rating icon 很棒

纯度: 99.02%

货号 T0285 别名 伊索昔康, Maxicam, Isoxicamum, IsoxicamoCas号 34552-84-6

Isoxicam (Isoxicamum) 是可口服的非甾体抗炎剂,可通过抑制环氧合酶 1 和 2 来阻断前列腺素的合成,可用于关节炎的研究。

规格价格库存数量
10 mg
¥ 132
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25 mg
¥ 189
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50 mg
¥ 289
现货
100 mg
¥ 479
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200 mg
¥ 739
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产品介绍


Isoxicam AI Summary
Isoxicam demonstrates a broad range of pharmacological and bioactivity profiles, including significant antiinflammatory effects, enzyme inhibition, and moderate antiviral activity. It exhibits antiinflammatory activity in models such as carrageenan-induced rat paw edema and adjuvant-induced polyarthritis, with effective doses ranging from 1.56 mg/kg to 12.5 mg/kg. The compound inhibits human Prostaglandin G/H synthase 2 and 1, with the highest inhibition observed at concentrations of 1 µg/mL and 10 µg/mL, respectively. Despite its high oral bioavailability and complete absorption in humans, it shows limited renal and hepatic clearance. Its total body clearance rate is 0.07 mL/min/kg, and it has a high volume of distribution at steady state, suggesting good tissue penetration. In vitro, Isoxicam is inactive against ovine COX-1 at 200 µM, but it shows various bioactivities such as modulating Lamin A splicing and inhibiting Ubiquitin-specific Protease USP2a, lipid storage, Histone Lysine Methyltransferase G9a, HP1-beta Chromodomain interactions, Polymerase Iota, and human tyrosyl-DNA phosphodiesterase 1 (TDP1). It also exhibits antiviral activities, including blocking Ebola virus entry and inhibiting SARS-CoV-2 induced cytotoxicity in both Caco-2 and VERO-6 cells. Pharmacokinetic studies reveal a mean residence time of 44 hours and a half-life of 33 hours after intravenous administration. Isoxicam binds strongly to human serum albumin (80.4% to 97.3%) and interacts with the binding sites, potentially displacing radiolabeled compounds. It inhibits sodium fluorescein uptake in OATP1B1 and OATP1B3-transfected cells and shows no significant inhibition of human BSEP, MRP2, MRP3, and MRP4. While Isoxicam demonstrates moderate activity in some assays, including inhibition of human HDAC6 and SARS-CoV-2 3CL-Pro protease, it is categorized as DILI negative according to the Drug Induced Liver Injury Prediction System. The overall profile indicates a compound with substantial antiinflammatory properties, broad enzyme inhibition capabilities, notable antiviral potential, and favorable pharmacokinetics and bioavailability..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Isoxicam (Isoxicamum) is a non-steroidal anti-inflammatory drug that is not marketed in the United States.
别名伊索昔康, Maxicam, Isoxicamum, Isoxicamo
化学信息
分子量335.34
分子式C14H13N3O5S
CAS No.34552-84-6
SmilesOC=1C=2C(S(=O)(=O)N(C)C1C(NC3=NOC(C)=C3)=O)=CC=CC2
密度1.588 g/cm3
颜色Yellow
物理性状Solid
储存&溶解度
存储store at low temperature | 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: 3.36 mg/mL (10.02 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.9820 mL14.9102 mL29.8205 mL149.1024 mL
5 mM0.5964 mL2.9820 mL5.9641 mL29.8205 mL
10 mM0.2982 mL1.4910 mL2.9820 mL14.9102 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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