產(chǎn)品目錄

規(guī)格	1mg 5mg 10mg 25mg
CAS	1492060-44-2
別名
化學(xué)名	2-[[4-chloro-6-[[4-(2-naphthalenyl)-2-thiazolyl]amino]-2-pyrimidinyl]thio]-octanoic acid
分子式	C25H25ClN4O2S
分子量	513.1
溶解度	≤20mg/ml in DMSO;25mg/ml in dimethyl formamide
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)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].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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