Impaired clearance of sunitinib leads to metabolic disorders and hepatotoxicity was written by Zhao, Qi;Zhang, Ting;Xiao, Xue-Rong;Huang, Jian-Feng;Wang, Yan;Gonzalez, Frank J.;Li, Fei. And the article was included in British Journal of Pharmacology in 2019.Recommanded Product: 1614-12-6 This article mentions the following:
Background and Purpose : Sunitinib is a small-mol. TK inhibitor associated with hepatotoxicity. The mechanisms of its toxicity are still unclear. Exptl. Approach : In the present study, mice were treated with 60, 150, and 450 mg·kg-1 sunitinib to evaluate sunitinib hepatotoxicity. Sunitinib metabolites and endogenous metabolites in liver, serum, faeces, and urine were analyzed using ultra-performance LC electrospray ionization quadrupole time-of-flight MS-based metabolomics. Key Results : Four reactive metabolites and impaired clearance of sunitinib in liver played a dominant role in sunitinib-induced hepatotoxicity. Using a non-targeted metabolomics approach, various metabolic pathways, including mitochondrial fatty acid β-oxidation (β-FAO), bile acids, lipids, amino acids, nucleotides, and tricarboxylic acid cycle intermediates, were disrupted after sunitinib treatment. Conclusions and Implications : These studies identified significant alterations in mitochondrial β-FAO and bile acid homeostasis. Activation of PPARa and inhibition of xenobiotic metabolism may be of value in attenuating sunitinib hepatotoxicity. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Recommanded Product: 1614-12-6).
1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Among the nitrogen-containing heterocyclic compounds, triazoles emerge with superior pharmacological applications. 1,2,3-Triazoles are usually prepared following (3+2) cycloaddition protocols. A common technique for unsubstituted triazoles is the Huisgen azide-alkyne 1,3-dipolar cycloaddition: a azide and an alkyne react at high temperature to form a ring. However, the Huisgen strategy produces a mixture of isomers (typically 1,4- and 1,5-disubstituted) when used to produce substituted triazoles.Recommanded Product: 1614-12-6
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics