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CAS No.: 72-48-0

茜素 Catalog No. CSN12906

Synonyms: 茜素

Alizarin strongly inhibits P450 isoform CYP1A1, CYP1A2 and CYP1B1 with IC50 of 6.2/10.0 and 2.7 μM respectively, weakly inhibits CYP2A6 and CYP2E1, and does not inhibit CYP2C19, CYP3A4 and CYP3A5.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Among human P450s, CYP1A1, CYP1A2, CYP1B1 and CYP3A4 are involved in bioactivation of carcinogens such as heterocyclic amines and polycyclic aromatic compounds. CYP1A2 is expressed constitutively in hepatic tissues where most carcinogens are metabolized. CYP1A1 is induced on treatment with Ah-receptor binding agents. CYP1B1 is widely distributed in human extrahepatic tissues, and it is constitutively expressed and is inducible by Ah-receptor ligands^[4]. Alizarin strongly inhibits the activities of CYP1A1, CYP1A2 and CYP1B1, with IC50 values of 6.2 μM, 10.0 μM and 2.7 μM, respectively, and weakly suppresses those of CYP2A6 and CYP2E1 in a dose-dependent manner, but do not inhibit those of CYP2C19, CYP3A4 and CYP3A5. CYP1B1 is the most strongly affected cytochrome P450 (CYP) molecule in a competitive manner by alizarin among CYPs examined in the study. The Km value of CYP1B1 is 11 μM, and the Ki value of alizarin against CYP1B1 is 0.5 μM^[4]. Alizarin suppressed the mutagenicity of MeIQx in TA1538 1A2/OR or 1B1/OR, which suggested that the antigenotoxic activities of alizarin can be explained by inhibition of CYP activities responsible for activating the mutagens^[4]. Alizarin was a very good antioxidant in their activity against iodophenol-derived phenoxyl radicals, superoxide anion radicals and lipid peroxidation in rat liver microsomes. In vivo experiment showed that alizarin reduced the hepatic content of thiobarbituric acid-reactive substances and lowered the serum level of alanine aminotransferase in poisoned animals ^[3].
动物研究
剂量
Rat: 20 mg/kg^[3] (i.m.); 100 mg/kg^[4] (i.p.), 200 mg/kg (i.p.)

给药途径
i.m.,i.p.
临床研究

动物研究
剂量	Rat: 20 mg/kg^[3] (i.m.); 100 mg/kg^[4] (i.p.), 200 mg/kg (i.p.)
给药途径	i.m.,i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03369457	-	-	Not yet recruiting	June 14, 2020	-
NCT03105284	Mesenchymal Stem Cells	Not Applicable	Completed	-	-
NCT02605603	-	-	Active, not recruiting	October 2018	United States, Virginia ... more >> O&O Alpan, LLC Fairfax, Virginia, United States, 22030 Collapse <<

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.1630 mL
- 20.8151 mL
- 41.6302 mL
- 5 mM
- 0.8326 mL
- 4.1630 mL
- 8.3260 mL
- 10 mM
- 0.4163 mL
- 2.0815 mL
- 4.1630 mL

技术信息

CAS号

72-48-0

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H8O4

运输

蓝冰

分子量

240.21

别名

茜素

溶解度

DMSO	100.0 mg/mL (416.3 mM)
Water	insoluble

动物实验配方

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