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N-(3-pyridyl)-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-(3-pyridyl)-Indomethacin amide图片
CAS NO:261766-29-4
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 No.261766-29-4
别名N-3PyIA
化学名N-(3-pyridyl)-1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetamide
Canonical SMILESClC1=CC=C(C(N2C(C=CC(OC)=C3)=C3C(CC(N([H])C4=CN=CC=C4)=O)=C2C)=O)C=C1
分子式C24H20ClN3O3
分子量433.9
溶解度≤3mg/ml in ethanol;3mg/ml in DMSO;3mg/ml in dimethyl formamide
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

N-(3-pyridyl)-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-(3-pyridyl)-indomethacin amide (N-3PyIA) is a reversible, potent and selective COX-2 inhibitor that inhibits human recombinant COX-2 and ovine COX-1 with IC50 values of 0.052 and >66 μM, respectively. It is over 1300 times less potent as an inhibitor of ovine COX-1. N-(3-pyridyl)-indomethacin amide is the 3-pyridyl amide derivative of indomethacin that shows selective against COX-2 [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.