Pirinixic Acid Aminothiazole (Synonyms:5-LO/mPGES1-IN-1)
目录号 : KCM11550 CAS No. : 1492060-44-2 纯度 : ≥98%
Microsomal prostaglandin E synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO) are key enzymes in the synthesis of PGE and leukotrienes (LTs), respectively. PGE and LTs are bioactive lipids that contribute to a broad range of pathologies, including inflammation and various forms of cancer. Pirinixic acid aminothiazole is a dual inhibitor of mPGES-1 and 5-LO (ICs = 0.4 and 0.2 µM, respectively). It is a weak inhibitor of COX-1 and -2 and has no effect on 12- and 15-LO isoforms. Pirinixic acid aminothiazole reduces the synthesis of PGE and LTC during zymosan-induced peritonitis in mice, resulting in a significantly diminished inflammatory response.
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生物活性

Pirinixic Acid Aminothiazole is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO). IC50 values are 0.3 and 0.4 μM, respectively. Pirinixic Acid Aminothiazole has anti-inflammatory activity.

体内研究

Pirinixic Acid Aminothiazole (10 mg/kg, intraperitoneal injection, pre-treatment 30 minutes before peritonitis induction) can reduce vascular permeability and inflammatory cell infiltration in a zymosan induced mouse peritonitis model, accompanied by impaired levels of cysteine leukotrienes and prostaglandin E2.

 

Animal Model: Zymosan-Induced Peritonitis in Mice
Dosage: 10 mg/kg
Administration: i.p. pretreated 30 minutes before peritonitis induction
Result: Reduced vascular permeability by 57% and inhibited neutrophil infiltration by 45%.
 
分子式
C25H25ClN4O2S2
分子量
513.1
CAS号
1492060-44-2
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
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