Nicotinamide-N-oxide-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENicotinamide N-oxideCat. No.: HY-101407CAS No.: 1986-81-8分式: CHNO分量: 138.12作靶点: CXCR; Drug Metabolite; Endogenous Metabolite作通路: GPCR/G Protein; Immunology/Inflammation; MetabolicEnzyme/Protease储存式: Powder -20C 3 years4C 2 years

2、In solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 6.6 mg/mL (47.78 mM; Need warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 7.2401 mL 36.2004 mL 72.4008 mL5 mM 1.4480 mL 7.2401 mL 14.4802 mL10 mM 0.7240 mL 3.6200 mL 7.2401 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVI

3、TY物活性 Nicotinamide N-oxide物体内烟酰胺分解代谢物,效选择性的CXCR2受体拮抗剂。IC50 & Target Human Endogenous Metabolite体外研究Nicotinamide is one of the forms of vitamin B3. It is a precursor for nicotinamide adenine dinucleotide, whichis best known as an electron carrier in oxidative phosphorylation and as a cofactor for man

4、y1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEdehydrogenases. It is metabolized through two enzymatic systems. The first system starts with themethylation of nicotinamide by nicotinamide N-methyltransferase, which can subsequently be oxidized byaldehyde oxidase. The second enzymatic system oxidi

5、zes nicotinamide to nicotinamide N-oxide 1. A seriesof nicotinamide N-oxides is synthesized and shown to be novel, potent, and selective antagonists of theCXCR2 receptor. Compound 1 has demonstrated potent inhibition of neutrophil chemotaxis (IC50=10 nM).Compound 2 is a selective antagonist of IL-8

6、binding (IC50=110 nM) and potent inhibitor of neutrophilchemotaxis (IC50=170 nM) 2.REFERENCES1. Real AM, et al. Nicotinamide N-oxidation by CYP2E1 in human liver microsomes. Drug Metab Dispos. 2013 Mar;41(3):550-3.2. Cutshall NS, et al. Nicotinamide N-oxides as CXCR2 antagonists. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1951-4.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: