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Pirfenidone

Catalog No. T2386   CAS 53179-13-8
Synonyms: S-7701,AMR-69, S-7701, AMR69

Pirfenidone (AMR69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production. Pirfenidone inhibits fibroblast, epidermal, platelet-derived, and transforming beta-1 growth factors, thereby slowing tumor cell proliferation. This agent also inhibits DNA synthesis and the production of mRNA for collagen types I and III, resulting in a reduction in radiation-induced fibrosis.

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Pirfenidone Chemical Structure
Pirfenidone, CAS 53179-13-8
Pack Size Availability Price/USD Quantity
25 mg In stock $ 30.00
50 mg In stock $ 39.00
100 mg In stock $ 57.00
200 mg In stock $ 73.00
500 mg In stock $ 97.00
1 g In stock $ 147.00
5 g In stock $ 217.00
1 mL * 10 mM (in DMSO) In stock $ 39.00
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Purity: 99.93%
Purity: 99.9%
Purity: 99.88%
Purity: 99.61%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Pirfenidone (AMR69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production. Pirfenidone inhibits fibroblast, epidermal, platelet-derived, and transforming beta-1 growth factors, thereby slowing tumor cell proliferation. This agent also inhibits DNA synthesis and the production of mRNA for collagen types I and III, resulting in a reduction in radiation-induced fibrosis.
In vitro Treatment with 0.5% Pirfenidone has been shown to reduce rat liver injury, a process linked to diminished proliferation of hepatic stellate cells and reduced collagen deposition. This treatment also leads to a 50-60% decrease in the transcription levels of procollagen α1(I), TIMP-1, and MMP-2 in rats induced with dimethylnitrosamine. In mice, Pirfenidone (250 mg/kg) significantly inhibits the production of pro-inflammatory cytokines including TNF-α, INF-γ, and IL-6, while promoting the production of the anti-inflammatory cytokine IL-10. In Sprague-Dawley rats on a low-sodium diet, Pirfenidone (250 mg/kg/day) ameliorates about 50% of cyclosporine-induced fibrosis and reduces the expression of TGF-β1 protein by 80%. Additionally, in ICR mice with bleomycin-induced pulmonary fibrosis receiving daily intravenous injections, Pirfenidone (400 mg/kg) suppresses HSP47-positive cells and myofibroblasts, key contributors to extracellular matrix accumulation.
In vivo In CCL-64 cells, Pirfenidone (< 5 mM) reduces TGF-β bioactivity by affecting the expression of TGF-β2 mRNA and the pro-TGF-β process. In LN-308 cells, Pirfenidone (< 8.3 mM) exhibits dose-dependent inhibition of recombinant plasminogen activator activity and MMP-11 expression. Across LN-18, T98g, LNT-229, and LN-308 cell lines, Pirfenidone (<10 mM) concentration-dependently decreases glioma cell density. In RAW264.7 cells, Pirfenidone (< 300 μg/mL) inhibits TNF-α through a translational mechanism, a process unrelated to the activation of mitogen-activated protein kinase 2, p38MAP kinase, and JNK.
Cell Research Pirfenidone (PFD) is dissolved in DMSO and stored, and then diluted with appropriate media before use[3]. HLECs are seeded in 96-well plates (1×104 cells/well) for 24 hours in α-MEM/10% FBS/1%NEAA, and are cultured in stationary tubes in serum-free medium for 24 hours. And then the culture medium is removed and cells are bathed in α-MEM with 10% FBS and 1% NEAA supplemented with 0, 0.01, 0.1, 0.2, 0.3, 0.5, or 1 mg/mL Pirfenidone for 0, 4, 12, 24, 48, or 72 hours. After incubation with 180 μL α-MEM and 20 μL of 5 mg/mL MTT for 4 hours at 37°C, the MTT solution is discarded. The Formosan precipitates are dissolved in 180 μL DMSO by agitating the dishes for 10 minutes at 200 rpm on an orbital shaker. The absorbance at 490 nm in each well is read with a micro plate reader. We further examined the effects of PFD by refining the concentrations at 0.2, 0.25, 0.3, 0.4, 0.5 and 0.6 mg/mL using the MTT assay[3].
Synonyms S-7701,AMR-69, S-7701, AMR69
Molecular Weight 185.22
Formula C12H11NO
CAS No. 53179-13-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100mg/ml (539.9mM)

H2O: 25 mg/ml (134.96mM)

TargetMolReferences and Literature

1. Nakazato H, et al. Eur J Pharmacol, 2002, 446(1-3), 177-185. 2. Burghardt I, et al. Biochem Biophys Res Commun, 2007, 354(2), 542-547. 3. Shihab FS, et al. Am J Transplant, 2002, 2(2), 111-119. 4. Kakugawa T, et al. Eur Respir J, 2004, 24(1), 57-65. 5. Di Sario A, et al. Dig Liver Dis, 2004, 36(11), 744-751.

TargetMolCitations

1. Hong M J, Hao M J, Zhang G Y, et al. Exophilone, a Tetrahydrocarbazol-1-one Analogue with Anti-Pulmonary Fibrosis Activity from the Deep-Sea Fungus Exophiala oligosperma MCCC 3A01264. Marine Drugs. 2022, 20(7): 448 2. Liang H X, Hao M J, Zhang G Y, et al.Lentinuses A–B, two alkaloids from the marine-derived fungus Lentinus sajor-caju with potent anti-pulmonary fibrosis activity.Fitoterapia.2023: 105433. 3. Tian J, Song D, Peng Y, et al.Silica-induced macrophage pyroptosis propels pulmonary fibrosis through coordinated activation of relaxin and osteoclast differentiation signaling to reprogram fibroblasts.Ecotoxicology and Environmental Safety.2024, 273: 116106.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Membrane Protein-targeted Compound Library Anti-Cancer Drug Library Inhibitor Library TGF-beta/Smad Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library EMA Approved Drug Library Drug-Fragment Library

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Keywords

Pirfenidone 53179-13-8 Immunology/Inflammation Microbiology/Virology Stem Cells CCR TGF-beta/Smad S-7701,AMR-69 AMR 69 CC chemokine receptor Transforming growth factor beta S 7701 S-7701 AMR-69 S7701 Inhibitor AMR69 inhibit inhibitor

 

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