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 > N-(2-phenylethyl)-Indomethacin amide
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:
 
N-(2-phenylethyl)-Indomethacin amide
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。
N-(2-phenylethyl)-Indomethacin amide图片
CAS NO:261766-32-9
规格:98%
分子量:461
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
inhibitor of COX-2
CAS:261766-32-9
分子式:C27H25ClN2O3
分子量:461
纯度:98%
存储:Store at -20°C

Background:

N-(2-phenylethyl)-Indomethacin amide is a reversible, potent and selective COX-2 inhibitor [1].


Cyclooxygenase (COX) is an enzyme responsible for formation of prostanoids, including thromboxane and prostaglandins such as prostacyclin. COX-1 is the constitutive isoform and is mainly responsible for the synthesis of cytoprotective prostaglandins in the gastrointestinal tract (GI) and of the proaggregatory thromboxane in blood platelets. COX-2 is inducible and short-lived that is stimulated by endotoxin, cytokines, and mitogens. COX-2 plays important roles in prostaglandin biosynthesis in inflammatory cells the central nervous system [1].


N-(2-phenylethyl)-Indomethacin amide (N-2PIA) is a reversible, potent and selective COX-2 inhibitor that inhibits human recombinant COX-2 and ovine COX-1 with IC50 values of 0.06 and >66 μM, respectively. It is over 1000 times less potent as an inhibitor of ovine COX-1. N-(2-phenylethyl)-Indomethacin amide is an analogous derivative of indomethacin that shows selective against COX-2 [1].


In the carageenan-induced foot pad edema assay, orally administration of N-2PIA showed anti-inflammatory activity [1].


Reference:
[1].  Kalgutkar AS, Marnett AB, Crews BC, et al. Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors. J Med Chem. 2000 Jul 27;43(15):2860-70.