您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > PPM-18
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
PPM-18
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PPM-18图片
CAS NO:65240-86-0
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
NF-κB inhibitor
Cas No.65240-86-0
别名NSC 73233
化学名N-(1,4-dihydro-1,4-dioxo-2-naphthalenyl)-benzamide
Canonical SMILESO=C(NC1=CC(=O)c2ccccc2C1=O)c1ccccc1
分子式C17H11NO3
分子量277.3
溶解度≥ 27.7mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PPM-18 is a chemically synthesized naphthoquinone derivative and an anti-inflammatory agent that inhibits the expression of inducible NO synthase (iNOS). NOS catalyzes the oxidation of the amino acid L-arginine to form NO. As an important cellular signaling molecule, NO has been implicated in modulating vascular tone, airway tone, insulinsecretion, and peristalsis. It has also been shown that NO is involved in angiogenesis and neural development and can function as a retrograde neurotransmitter

In vitro: Pretreatment of rat alveolar macrophages with PPM-18 (0.1-10 μM) significantly inhibited nitrite production, iNOS mRNA accumulation and iNOS protein expression. PPM-18 did not affect the enzymic activities of iNOS and other constitutive NOS forms directly. PPM-18 (10 μM) inhibited the LPS-induced increase in nuclear transcription factor κB (NF-κB) p65 and p50 in nucleus.. PPM-18 significantly decreased LPS-induced the production of tumour necrosis factor α [1]. PPM-18 inhibited NF-κB activation with an IC50 of 5 μM [3].

In vivo: In rats, intravenously pretreatment with PPM-18 (15 mg/kg) maintained a significantly higher mean arterial pressure compared with LPS-treated controls. PPM-18 protected mice against LPS-induced lethal toxicity. In mice, PPM-18 (5 or 15 mg/kg) dose-dependently decreased the lethality. In the mouse model of sepsis, PPM-18 exhibited as a potent inhibitor of iNOS expression by blocking the binding of NF-κB to promoter and exerted a beneficial effect [1].

References:
[1] YU M S, LIN J F W U T L, KUO C S.  Inhibition of nitric oxide synthase expression by PPM-18, a novel anti-inflammatory agent, in vitro and in vivo[J]. Biochemical Journal, 1997, 328(2): 363-369.
[2] Beck K F, Eberhardt W, Frank S, et al.  Inducible NO synthase: role in cellular signalling[J]. Journal of Experimental Biology, 1999, 202(6): 645-653.
[3] Davis, M. E.,Grumbach, I.M.,Fukai, T., et al. Shear stress regulates endothelial nitric-oxide synthase promoter activity through nuclear factor κB binding.The Journal of Biological Chemisty 279(1), 163-168 (2004).