Nicotinamide N-oxide是生物体内烟酰胺分解代谢物,是高效选择性CXCR2受体拮抗剂。
产品描述
Nicotinamide N-oxide is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. The enzyme that catalyzes the reduction of nicotinamide N-oxide to nicotinamide in the liver is xanthine oxidase.
体外活性
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[1]. 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)[2].
Cas No.
1986-81-8
分子式
C6H6N2O2
分子量
138.126
别名
1-oxynicotinamide;N-氧代烟酰胺;Nicotinamide-N-oxide;烟酰胺-N-氧化物;Nicotinamide 1-oxide
储存和溶解度
DMSO:8 mg/mL(57.9 mM)
H2O:Limited solubility
Powder: -20°C for 3 years
In solvent: -80°C for 2 years