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.
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.