Name: Pirinixic Acid Aminothiazole
Price: 231.00 USD

- Overview
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    Background
    
    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].
    
    [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.
- Properties
  - Alternative Name
    
    2-[[4-chloro-6-[[4-(2-naphthalenyl)-2-thiazolyl]amino]-2-pyrimidinyl]thio]-octanoic acid
    
    CAS Number
    
    1492060-44-2
    
    Molecular Formula
    
    C25H25ClN4O2S
    
    Molecular Weight
    
    513.1
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤20mg/ml in DMSO;25mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Pirinixic Acid Aminothiazole

Pirinixic Acid Aminothiazole

Background

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