Shelf life (days): 730.0
Formulation: A solid
Formal Name: 5-methyl-1-(phenyl-2,3,4,5,6-d5)-2(1H)-pyridinone
Purity: ≥99% deuterated forms (d1-d5)
Formula Markup: C12H6D5NO
Formula Weight: 190.25218
CAS Number: 1020719-62-3
Notes: Pirfenidone-d5 is intended for use as an internal standard for the quantification of pirfenidone (Item No. 13986) by GC- or LC-MS. 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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