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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Cited by 13 Publications

3 Customer Reviews

  • 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.

  • (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, 57(1):77-90. Pirfenidone purchased from Selleck.

  • Immunofluorescence staining of myosin (red) when TGFb2 and TGFb3 were inhibited using pirfenidone. Nucleus was stained with DAPI (blue) Scale bars: 200 μm. Magnification: 100×.

    Aging Cell, 2018, doi: 10.1111/acel.12788. Pirfenidone purchased from Selleck.

Purity & Quality Control

Choose Selective TGF-beta/Smad Inhibitors

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HFL1 cells M4m5OGZ2dmO2aX;uJIF{e2G7 MlnQOFghcA>? NULvOo96SW62aX\pZpJwfGmlIHHjeIl3cXS7IHnuJGhHVDFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuII\pZYJqdGm2eTDh[pRmeiB2ODDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfS=> MWCyOlg6PjdyNx?=
LNCaP Ml3XR4VtdCCpcn;3eIgh[XO|YYm= NEPkOmUxNCByLkGsJFAvOyCvZz;tcC=> NX:1O|Q3OyCmYYnz NXfTSpF3WE[GIITy[YF1dWWwdDDzbYdvcW[rY3HueIx6KHO3cIDy[ZN{\WRidHjlJIdzd3e2aDDv[kBk\WyuczDheEAxNjNibXevcYw> M1jNTVMxPjJzMUe1
PC-3 MXzD[YxtKGe{b4f0bEBie3OjeR?= M2HSNVAtKDBwMTygNE4{KG2pL33s MVOzJIRigXN? NYPxNJJ7WE[GIITy[YF1dWWwdDDzbYdvcW[rY3HueIx6KHO3cIDy[ZN{\WRidHjlJIdzd3e2aDDv[kBk\WyuczDheEAxNjNibXevcYw> NEixN3A{ODZ{MUG3OS=>
E9 MmPxR4VtdCCpcn;3eIgh[XO|YYm= MVmwMEAxNjFuIECuN{Bu\y:vbB?= MojrN{Bl[Xm| MoDiVGZFKHS{ZXH0cYVvfCC|aXfubYZq[2GwdHz5JJN2eHC{ZYPz[YQhfGinIHfyc5d1cCCxZjDj[YxteyCjdDCwMlMhdWdxbXy= NG\SVlk{ODZ{MUG3OS=>
F10 MmjrR4VtdCCpcn;3eIgh[XO|YYm= Mnq4NEwhOC5zLDCwMlMhdWdxbXy= NH:0O5o{KGSjeYO= M1S3VXBHTCC2cnXheI1mdnRic3nncolncWOjboTsfUB{fXCycnXzd4VlKHSqZTDndo94fGhib3[gZ4VtdHNiYYSgNE4{KG2pL33s MX6zNFYzOTF5NR?=
AIDL NILOb5BE\WyuIHfyc5d1cCCjc4PhfS=> NEXOWIIxNCByLkGsJFAvOyCvZz;tcC=> MojFN{Bl[Xm| MV7QSmQhfHKnYYTt[Y51KHOrZ37p[olk[W62bImgd5VxeHKnc4Pl[EB1cGViZ4Lve5RpKG:oIHPlcIx{KGG2IECuN{Bu\y:vbB?= MX6zNFYzOTF5NR?=
human intestinal fibroblasts (HIFs) M1TwNmZ2dmO2aX;uJIF{e2G7 NFHyc5UyKGh? M2r6bnBHTCCrbnjpZol1eyCKSV\zJIRq\m[ncnXueIlifGmxbjDhcoQhfGinIHPvcIxi\2WwIHTldI9{cXSrb36gbY5lfWOnZDDifUBVT0ZvzsKxMi=> NX7wVo9wOzBzNUK4OFg>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Immunofluorescence
α-SMA; 

PubMed: 22132230     


Effects of 1.0 or 1.5 mg/ml pirfenidone on α-SMA expression and morphological changes of CFs (Cardiac fibroblasts) were determined by immunofluorescence staining with anti-α-SMA antibody. Scale bar = 50.0 µm. 

SMAD4 / SMAD2 / SMAD3 ; 

PubMed: 23437252     


After stimulated by 12.5 ng/ml TGF-β2 for 24 hours, the staining of nuclei SMAD4 (green) enhanced when that of SMAD4 in the cytoplasm were weakened, and SMAD2/3 proteins (red) were assembled on the nuclear membrane and some of them entered the nuclei. Expression of nuclei SMAD2/3 and SMAD4 were depressed after treatment with 0.5 mg/ml pirfenidone. The nuclei stained by DAPI (blue). Magnification, ×1000.

F-actin / β-catenin / Vimentin ; 

PubMed: 29325547     


Immunofluorescence staining showed that treatment with SB or PFD increased E-cadherin levels, decreased vimentin and nuclear β-catenin distribution in MCF-7 and MDA-MB-231 cells. CAFs promoted F-actin polymerization and stability in cancer cells, whereas treatment with SB or PFD impaired the formation of stress fibers. Scale bar: 15 μm

22132230 23437252 29325547
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 to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
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
in solvent
Synonyms S-7701,AMR-69

Bio Calculators

Molarity Calculator

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Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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The Serial Dilution Calculator Equation

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03981094 Recruiting Drug: BMS-986278|Drug: Pirfenidone Idiopathic Pulmonary Fibrosis (IPF) Bristol-Myers Squibb May 6 2019 Phase 1
NCT03692481 Not yet recruiting Radiation: 18FDG-PET scan Idiopathic Pulmonary Fibrosis Assistance Publique - Hôpitaux de Paris April 30 2019 Not Applicable
NCT03958071 Completed Drug: Nintedanib|Drug: Pirfenidone|Other: Untreated Cohort Idiopathic Pulmonary Fibrosis Boehringer Ingelheim December 19 2018 --
NCT03725852 Recruiting Drug: GLPG1205|Drug: Placebo Idiopathic Pulmonary Fibrosis Galapagos NV September 27 2018 Phase 2
NCT03567785 Recruiting -- Idiopathic Pulmonary Fibrosis|Pulmonary Fibrosis KU Leuven July 17 2018 --
NCT03473340 Recruiting Drug: Pirfenidone Capsule|Drug: Placebo Capsule Disorder Related to Lung Transplantation|Chronic Lung Allograft Dysfunction University of Michigan|Genentech Inc. April 27 2018 Phase 2

Tech Support

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.

Handling Instructions

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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.

TGF-beta/Smad Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID