Pirfenidone

Pirfenidone is an orally bioavailable pyridone derivative with antifibrotic, anti-inflammatory, and antioxidant activities. It inhibits TGF-beta1-stimulated increases in collagen type I, fibronectin, and Hsp47 expression in A549 lung cancer cells in a concentration-dependent manner. 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 (Cay-13877). 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. Pirfenidone also inhibits NADPH-dependent lipid peroxidation in sheep liver microsomes and scavenges hydroxyl radicals (IC50s = ~6 and ~2.5 mM, respectively). Formulations containing pirfenidone have been used in the treatment of idiopathic pulmonary fibrosis.Formal Name: 5-methyl-1-phenyl-2(1H)-pyridinone. CAS Number: 53179-13-8. Synonyms: AMR 69. Molecular Formula: C12H11NO. Formula Weight: 185.2. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 17 mg/ml, Ethanol: 20 mg/ml, PBS (pH 7.2): 3 mg/ml. lambdamax: 203, 223, 319 nm. SMILES: CC(C=C1)=CN(C2=CC=CC=C2)C1=O. InChi Code: InChI=1S/C12H11NO/c1-10-7-8-12(14)13(9-10)11-5-3-2-4-6-11/h2-9H,1H3. InChi Key: ISWRGOKTTBVCFA-UHFFFAOYSA-N.