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Nicotinamide N-oxide

CAS No. : 1986-81-8

MCE 国际站：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。

研究领域：GPCR/G Protein  |  Immunology/Inflammation  |  Metabolic Enzyme/Protease

作用靶点：CXCR  |  Drug Metabolite  |  Endogenous Metabolite

结构分类：生物碱  |  吡啶类生物碱

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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