|Posted on:||3 February 2018 / 02:22|
Other Name: 5-Methyl-N-phenyl-2-1H-pyridone
Appearance: White crystal powder
Melting point: 102–109
Solubility: DMSO: 10 mg/mL, soluble
Loss on drying <1.0%
Known single impurity <1.0%
Unknown single impurity <0.5%
Total impurity <2.0%
Assay(as dried) 99%min
MF : C12H11NO
Pirfenidone is an anti-inflammatory drug used to treat idiopathic pulmonary fibrosis.Antifibrotic agent, effective in models of pulmonary and lung fibrosis. Inhibits collagen production and fibroblast proliferation. Regulates cytokine levels following oral administration in vivo. Potent scavenger of free radicals and inhibitor of lipid peroxidation.Pirfenidone inhibits collagen production and fibroblast proliferation. It has shown antifibrotic and anti-inflammatory properties in variety of animal models of pulmonary fibrosis, and in clinical trials.
In vitro, pirfenidone can inhibit the uterine flesh tumour cells and leiomyoma cells proliferation. Pirfenidone can inhibit the TGF – beta – 1 inducing fibroblast collagen formation. Inhibition of PDGF, FGF and TGF – beta – 1 inducing fibroblast proliferation. In hamster model, pirfenidone, taken by mouth, that can the prevention and treatment of pulmonary fibrosis induced by bleomycin. Pirfenidone can prevent the sclerosing peritonitis in rats induced by chemical, can also be keloid grafting for the treatment of nude mice. Pirfenidone 0.01 1 mg/ml can suppress the matrix and dose dependent manner serum stimulate uterine fibroids and leiomyoma cell DNA synthesis, the compound has no cytotoxic effect, has no effect on collagen mRNA level also. Pirfenidone in hamster pulmonary fibrosis model can reduce the disease before the collagen I mRNA level enhancement, reduce the level of the lung hydroxyproline and malondialadehyde and lung preserved ammonia acyl hydroxylase activity.
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