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Ketorolac

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纯度: 99.68%

货号 T21412Cas号 74103-06-3

别名 酮咯酸, Toradol, Sprix, Macril, Acuvail, Acular

Ketorolac (Acuvail) 是非甾体抗炎剂,是非选择性的COX 抑制剂,对 COX-1 和 COX-2 的IC50值分别为 20 和 120 nM。

Ketorolac

Ketorolac

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Rating icon 很棒

纯度: 99.68%

货号 T21412 别名 酮咯酸, Toradol, Sprix, Macril, Acuvail, AcularCas号 74103-06-3

Ketorolac (Acuvail) 是非甾体抗炎剂,是非选择性的COX 抑制剂,对 COX-1 和 COX-2 的IC50值分别为 20 和 120 nM。

规格价格库存数量
100 mg
¥ 133
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500 mg
¥ 278
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1 g
¥ 392
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2 g
¥ 579
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5 g
¥ 963
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10 g
¥ 1,420
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1 mL x 10 mM (in DMSO)
¥ 147
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产品介绍


Ketorolac AI Summary
Ketorolac demonstrates a wide array of bioactivities including significant anti-inflammatory and analgesic effects at various dosages. Specifically, it inhibits carrageenan-induced edema in rats at 15 mg/kg, phenylquinone-induced writhing in mice at 70 mg/kg, cotton pellet granuloma in mice at 0.5 mg/kg, and adjuvant-induced arthritis in rats at 2.0 mg/kg. However, it also induces chronic gastrointestinal erosive activity in rats at 5.0 mg/kg. The therapeutic ratio of gastrointestinal erosion to anti-inflammatory activity in rat paw is 18.0, suggesting a favorable balance. Pharmacokinetic studies show that Ketorolac has high oral bioavailability (≥80%), rapid absorption with a Tmax of 1 hour, and moderate systemic clearance. It exhibits high plasma protein binding (99.2%) and moderate lipophilicity (LogP ~2.7). Specific enzyme inhibition includes COX-1 with an IC50 of 13.0 nM, COX-2 with an IC50 of 424.0 nM, and prostaglandin synthetase activity in mouse brain microsomes with an IC50 of 230.0 nM. Ketorolac also demonstrates properties such as a moderate pKa of 3.49, acceptable chemical stability, and diverse bioactivities including potential antiviral and antihyperalgesic effects. Despite its therapeutic potential, Ketorolac shows moderate risk for liver toxicity and gastrointestinal side effects, with an ulcerogenic effect comparable to ketorolac and a notable liver toxicity severity score. Overall, Ketorolac is a potent anti-inflammatory and analgesic agent with a complex pharmacological profile, necessitating careful consideration of its side effects in therapeutic applications..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Ketorolac (Acuvail) is a non-steroidal anti-inflammatory drug (NSAID) in the family of heterocyclic acetic acid derivatives. It acts by inhibiting the bodily synthesis of prostaglandins.
靶点活性
COX-1:20 nM, COX-2:120 nM 
别名酮咯酸, Toradol, Sprix, Macril, Acuvail, Acular
化学信息
分子量255.27
分子式C15H13NO3
CAS No.74103-06-3
SmilesOC(=O)C1CCN2C1=CC=C2C(=O)C1=CC=CC=C1
密度1.398 g/cm3
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: 45 mg/mL (176.28 mM), Sonication is recommended.
H2O: 70 mg/mL (274.22 mM), Sonication is recommended.
溶液配制表
DMSO/H2O
1mg5mg10mg50mg
1 mM3.9174 mL19.5871 mL39.1742 mL195.8710 mL
5 mM0.7835 mL3.9174 mL7.8348 mL39.1742 mL
10 mM0.3917 mL1.9587 mL3.9174 mL19.5871 mL
20 mM0.1959 mL0.9794 mL1.9587 mL9.7936 mL
50 mM0.0783 mL0.3917 mL0.7835 mL3.9174 mL
100 mM0.0392 mL0.1959 mL0.3917 mL1.9587 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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