An orally bioavailable pyridone derivative with antifibrotic

Pirfenidone – 50 mg

Brand:
Cayman
CAS:
53179-13-8
Storage:
-20
UN-No:
Non-Hazardous - /

Pirfenidone is an orally bioavailable pyridone derivative with antifibrotic, anti-inflammatory, and antioxidant activities.{42405,42406,42407,21821,21616} It inhibits TGF-β1-stimulated increases in collagen type I, fibronectin, and Hsp47 expression in A549 lung cancer cells in a concentration-dependent manner.{21821} Pirfenidone (300 mg/kg per day) inhibits fibrosis and inhibits increases in collagen content, fibrocyte pool size, and the levels of chemokines CCL2 and CCL12 in lung in a mouse model of pulmonary fibrosis induced by bleomycin (Item No. 13877).{42406} In a mouse model of non-alcoholic steatohepatitis (NASH), pirfenidone inhibits fibrosis and increases in hepatocyte apoptosis, lobular inflammation, and hepatic expression of the fibrosis-related genes Col1a1, Timp1, Tgfb1, Pdgfb, and Fgf2 when administered at a dose of 280 mg/kg but has no effect on steatosis.{42405} Pirfenidone also inhibits NADPH-dependent lipid peroxidation in sheep liver microsomes and scavenges hydroxyl radicals (IC50s = ~6 and ~2.5 mM, respectively).{42407} Formulations containing pirfenidone have been used in the treatment of idiopathic pulmonary fibrosis.  

 

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An orally bioavailable pyridone derivative with antifibrotic, anti-inflammatory, and antioxidant activities; inhibits TGF-β1-stimulated increases in collagen type I, fibronectin, and Hsp47 expression in A549 lung cancer cells in a concentration-dependent manner; inhibits fibrosis and inhibits increases in collagen content, fibrocyte pool size, and the levels of chemokines CCL2 and CCL12 at 300 mg/kg in lung in a mouse model of pulmonary fibrosis induced by bleomycin; inhibits fibrosis and increases in hepatocyte apoptosis, lobular inflammation, and hepatic expression of the fibrosis-related genes Col1a1, Timp1, Tgfb1, Pdgfb, and Fgf2 in a mouse model of NASH at 280 mg/kg; inhibits NADPH-dependent lipid peroxidation in sheep liver microsomes and scavenges hydroxyl radicals (IC50s = ~6 and ~2.5 mM, respectively)

Formal name: 5-methyl-1-phenyl-2(1H)-pyridinone

Synonyms:  AMR 69

Molecular weight: 185.2

CAS: 53179-13-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ox Stress Reagents|Antioxidants||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH||Research Area|Immunology & Inflammation||Research Area|Oxidative Stress & Reactive Species|Antioxidant Activity||Research Area|Oxidative Stress & Reactive Species|Lipid Peroxidation||Research Area|Oxidative Stress & Reactive Species|Reactive Oxygen|Non-enzymatic

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