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Pirfenidone
- AMR-69
- Soluble in DMSO
- MF: C12H11NO
- MW: 185.22
Description
Pirfenidone (AMR-69) is an orally available agent with therapeutic potential for idiopathic pulmonary fibrosis (IPF) with and IC50 value of 14.44 mM for inhibition of cell proliferation against MRC-5 cells. Pirfenidone 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.
Antifibrotic pharmacology is essential to understanding progressive disease models like IPF. As a chemical probe, Pirfenidone supports mechanistic studies of anti-inflammatory pathways in diverse biochemical, cellular, and in vivo assays.
Key Features
- Dual antifibrotic and anti-Inflammatory profile
- Inhibits the expression and downstream Smad activation of TGF-β
- Supports suppression of myofibroblast differentiation
- Probe for progressive disease models such as IPF
Applications
- Anti-inflammatory/anti-fibrosis pharmacology and target-validation studies
- Cytokine and Inflammatory Pathway Probing
- Disease-model research related to fibrosis, IPF modeling
- Multi-Organ Fibrosis/ECM Deposition Profiling
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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