Pirfenidone

Catalog No.S2907 Synonyms: S-7701,AMR-69

Pirfenidone Chemical Structure

Molecular Weight(MW): 185.22

Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Phase 3.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 270 In stock
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2 Customer Reviews

  • (E, F) Western Blot analysis of phLF isolated from (E) IPF patients or (F) donors treated for 48h with increasing concentrations of nintedanib (0.01, 0.1, 1 μM) or pirfenidone (100, 500, 1000 μM) in absence or presence of TGF-β1 (2 ng/mL). Densitometric analysis and representative blots show the effect of nintedanib and pirfenidone on collagen I (Col I) protein expression relative to β-actin as loading control (ACTB). Data are based on 8 (IPF) or 3 (donor) completely independent experiments and are given as mean ± SEM. Statistical significance between control and different concentrations of nintedanib or pirfenidone is indicated by horizontal brackets and asterisks.

    Am J Respir Cell Mol Biol, 2017. Pirfenidone purchased from Selleck.

    Ex vivo tissue spotting experiment of pirfenidone dilutions and MalDI imagingn approach of in vivo administered pirfenidone measured with MalDI-TOF mass spectrometer. ex vivo dilution series of pirfenidone (m/z 186.2?.1 Da) covered with CHCa matrix. In vivo treated liver cryosections measured by MalDI-TOF imaging using CHCa. Size bar corresponds to 2 mm.

    Histochem Cell Biol 2014 142(4), 361-71. Pirfenidone purchased from Selleck.

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Biological Activity

Description Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Phase 3.
Targets
TGF-β [2]
(Cell-free assay)
In vitro

Pirfenidone (< 300 μg/mL) suppresses the proinflammatory cytokine tumor necrosis factor-α (TNF-α) by a translational mechanism in RAW264.7 cells, which is independent of activation of the mitogen-activated protain kinase (MAPK) 2, p38 MAP kinase, and c-Jun N-terminal kinase (JNK). [1] Pirfenidone (< 10 mM) leads to reduced glioma cell density in concentration-dependent manner in LN-18, T98G, LNT-229 and LN-308 cell lines. Pirfenidone (< 5 mM) reduces TGF-β bioactivity by affecting TGF-β2 mRNA expression and processing of pro-TGF-β in CCL-64 cells. Pirfenidone (< 8.3 mM) inhibits the activity of recombinant furin and downregulates the expression of MMP-11 in a dose-dependent manner in LN-308 cells. [2]

In vivo Pirfenidone (250 mg/kg) potently inhibits the production of the proinflammatory cytokines, TNF-alpha, interferon-gamma, and interleukin-6, but enhances the production of the anti-inflammatory cytokine, interleukin-10, in mice. [1] Pirfenidone (250 mg/kg/day) ameliorates cyclosporine-induced fibrosis by about 50% and decreases TGF-beta1 protein expression by 80% in Sprague-Dawley rats receiving a low-salt diet. [3] Pirfenidone (400 mg/kg/day) inhibits heat shock protein 47-positive cells and myofibroblasts, the principal cells responsible for the accumulation and deposition of extracellular matrix seen in pulmonary fibrosis in ICR mice intravenously injected with bleomycin. [4] Pirfenidone (0.5%, liquid diet) treatment reduces the degree of liver injury in rats, as determined by alanine aminotransferase values and necro-inflammatory score, which is associated with reduced hepatic stellate cells proliferation and collagen deposition. Pirfenidone (0.5%, liquid diet) administration downregulates dimethylnitrosamine induced transcripts levels of procollagen alpha1(I), TIMP-1 and MMP-2 by 50-60% in rats, and this is associated with a 70% reduction in collagen deposition. [5]

Protocol

Animal Research:[3]
+ Expand
  • Animal Models: Sprague-Dawley rats receiving a low-salt diet
  • Formulation: saline
  • Dosages: 250 mg/kg
  • Administration: oral diet
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 37 mg/mL (199.76 mM)
Ethanol 37 mg/mL (199.76 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+ddH2O
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 185.22
Formula

C12H11NO

CAS No. 53179-13-8
Storage powder
Synonyms S-7701,AMR-69

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00332033 Completed Uterine Leiomyoma|Fibroids Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|National Institutes of Health Clinical Center (CC) May 25, 2006 Phase 2
NCT02932566 Not yet recruiting Cardiac Failure University Hospital of South Manchester NHS Foundation Trust|National Institute for Health Research, United Kingdom|University of Manchester|University of Liverpool, Clinical Trials Research Centre|Roche Therapeutics Ltd January 2017 Phase 2
NCT02808871 Not yet recruiting Rheumatoid Arthritis Interstitial Lung Disease Ivan O. Rosas|Brigham and Womens Hospital January 2017 Phase 2
NCT02951429 Recruiting Idiopathic Pulmonary Fibrosis Hoffmann-La Roche December 2016 Phase 2
NCT02958917 Not yet recruiting Interstitial Lung Disease National Jewish Health|Genentech, Inc. December 2016 --
NCT02823236 Not yet recruiting Keloid Centro Dermatológico Dr. Ladislao de la Pascua|Grupo Medifarma, S. A. de C. V. August 2016 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    I'd like to know how to use your 50mg dose pirfenidone to make a solution for intraperitoneal injection in a mouse. Could you give me some advice?

  • Answer:

    For I.P. injection, S2907 Pirfenidone can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 10 mg/ml clearly. When preparing the solution, please dissolve the compound in DMSO clearly first. Then add PEG, after they mixed well, then dilute with water.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID