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Pirinixic Acid Aminothiazole
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。
Pirinixic Acid Aminothiazole图片
CAS NO:1492060-44-2
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
dual inhibitor of mPGES-1 and 5-LO
Cas No.1492060-44-2
化学名2-[[4-chloro-6-[[4-(2-naphthalenyl)-2-thiazolyl]amino]-2-pyrimidinyl]thio]-octanoic acid
Canonical SMILESClC1=NC(SC(CCCCCC)C(O)=O)=NC(NC2=NC(C3=CC=C(C=CC=C4)C4=C3)=CS2)=C1
分子式C25H25ClN4O2S
分子量513.1
溶解度≤20mg/ml in DMSO;25mg/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

Pirinixic Acid Aminothiazole is a dual inhibitor of 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase 1 (mPGES-1) with IC50 values of 0.3 and 0.4 μM, respectively [1].

5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1) are critical enzymes involved in the metabolism of arachidonic acid (AA). They are key enzymes in the synthesis of leukotrienes (LTs) and PGE2, respectively [1][2][3]. Dual inhibition of 5-LO and mPGES-1 is currently pursued as potential pharmacological strategy for treatment of inflammation and cancer [1].

Pirinixic Acid Aminothiazole is a dual inhibitor of 5-LO and mPGES-1. Pirinixic Acid Aminothiazole hardly inhibited cyclooxygenase (COX)-1/2 activities and failed to inhibit 12/15-LOs. In cell-free assay, Pirinixic Acid Aminothiazole was highly potent against both 5-LO and mPGES-1 with IC50 values of 0.3 and 0.4 μM, respectively. In the cell-based assay, Pirinixic Acid Aminothiazole inhibited 5-LO directly with IC50 value of 0.2 μM [1].

In zymosan-induced peritonitis in mice, Pirinixic Acid Aminothiazole (10 mg/kg) reduced vascular permeability by 57% and inhibited neutrophil infiltration by 45%, accompanied by significantly impaired levels of cysLTs (84% reduction) and PGE2 (46% reduction). These results suggested that Pirinixic Acid Aminothiazole dually inhibited LT and PGE2 synthesis in vivo connected to anti-inflammatory effectiveness [1].

References:
[1].  Hanke T, Dehm F, Liening S, et al. Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo. J Med Chem. 2013 Nov 27;56(22):9031-44.
[2].  Funk CD. Prostaglandins and leukotrienes: advances in eicosanoid biology. Science. 2001 Nov 30;294(5548):1871-5.
[3].  Samuelsson B, Morgenstern R, Jakobsson PJ. Membrane prostaglandin E synthase-1: a novel therapeutic target. Pharmacol Rev. 2007 Sep;59(3):207-24.