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Pirfenidone
- AMR-69
- Soluble in DMSO
- MF: C12H11NO
- MW: 185.22
Description
Orally available agent with therapeutic potential for idiopathic pulmonary fibrosis (IPF; IC50 value 14.44 mM for inhibition of cell proliferation against MRC-5 cells) that has combined anti-inflammatory, antioxidant and antifibrotic effects in experimental models of pulmonary fibrosis. Mechanistically, Pirfenidone inhibits not only TGF-β-induced Smad3, p38 and Akt phosphorylation in human lung fibroblasts (HLFs), but also significantly increased RGS2 mRNA and protein expression in fibroblasts.
More Information
| Parent CAS No. | 53179-13-8 |
|---|---|
| Chemical Name | 5-methyl-1-phenylpyridin-2(1H)-one |
| SMILES | C1(=O)N(C2=CC=CC=C2)C=C(C)C=C1 |
| MFCD | MFCD00866047 |
| InChi | InChI=1S/C12H11NO/c1-10-7-8-12(14)13(9-10)11-5-3-2-4-6-11/h2-9H,1H3 |
| InChiKey | ISWRGOKTTBVCFA-UHFFFAOYSA-N |
| CID | 40632 |
| Short Description | anti-inflammatory/anti-fibrosis agent |
References
- Z Ma et al. Synthesis and biological evaluation of the pirfenidone derivatives as antifibrotic agents. Bioorg Med Chem Lett. 2014 Jan 1;24(1):220-3.
- E Conte et al. Effect of pirfenidone on proliferation, TGF-β-induced myofibroblast differentiation and fibrogenic activity of primary human lung fibroblasts. Eur J Pharm Sci. 2014 Jul 16;58:13-9.
- Y Xie et al. Upregulation of RGS2: a new mechanism for pirfenidone amelioration of pulmonary fibrosis. Respir Res. 2016 Aug 22;17(1):103.
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