耗材描述
Nicotinamide N-oxide
产品活性:Nicotinamide N-oxide是生物体内烟酰胺分解代谢物, 是高效选择性的CXCR2受体拮抗剂。
产品来源: https://www.medchemexpress.cn/Nicotinamide_N-oxide.html
研究领域:GPCR/G Protein | Immunology/Inflammation | Metabolic Enzyme/Protease
作用靶点:Oxidative Phosphorylation | CXCR | Drug Metabolite | Endogenous Metabolite
结构分类:生物碱 | 吡啶类生物碱 | 结构分类
In Vitro: Nicotinamide is one of the forms of vitamin B3. It is a precursor for nicotinamide adenine dinucleotide, which is best known as an electron carrier in oxidative phosphorylation and as a cofactor for many dehydrogenases. It is metabolized through two enzymatic systems. The first system starts with the methylation of nicotinamide by nicotinamide N-methyltransferase, which can subsequently be oxidized by aldehyde oxidase. The second enzymatic system oxidizes nicotinamide to nicotinamide N-oxide. A series of nicotinamide N-oxides is synthesized and shown to be novel, potent, and selective antagonists of the CXCR2 receptor. Compound 1 has demonstrated potent inhibition of neutrophil chemotaxis (IC50=10 nM). Compound 2 is a selective antagonist of IL-8 binding (IC50=110 nM) and potent inhibitor of neutrophil chemotaxis (IC50=170 nM).
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