Pirfenidone (S-7701)

For research use only.

Catalog No.S2907 Synonyms: AMR-69

33 publications

Pirfenidone (S-7701) Chemical Structure

CAS No. 53179-13-8

Pirfenidone (S-7701, AMR-69) 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. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.

Size Price Stock Quantity  
10mM (1mL in DMSO) RMB 731.52 In stock
RMB 568.87 In stock
RMB 2218.54 In stock
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Selleck's Pirfenidone (S-7701) has been cited by 33 publications

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Biological Activity

Description Pirfenidone (S-7701, AMR-69) 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. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. 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 NH3pdXBHfW6ldHnvckBie3OjeR?= NIXSOmU1QCCq MmXsRY51cW[rYoLveIlkKGGldHn2bZR6KGmwIFjGUFEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygTWM2OCB;IECuO|Eh|ryPLh?= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh7NkewO{c,OjZ6OU[3NFc9N2F-
LNCaP NGrQ[FBE\WyuIHfyc5d1cCCjc4PhfS=> NXvsbnV3OCxiMD6xMEAxNjNibXevcYw> NGrGXo8{KGSjeYO= NX;yUVdSWE[GIITy[YF1dWWwdDDzbYdvcW[rY3HueIx6KHO3cIDy[ZN{\WRidHjlJIdzd3e2aDDv[kBk\WyuczDheEAxNjNibXevcYw> NFjpOIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|ME[yNVE4PSd-M{C2NlEyPzV:L3G+
PC-3 MVLD[YxtKGe{b4f0bEBie3OjeR?= MW[wMEAxNjFuIECuN{Bu\y:vbB?= NXfyOVc3OyCmYYnz Mn[2VGZFKHS{ZXH0cYVvfCC|aXfubYZq[2GwdHz5JJN2eHC{ZYPz[YQhfGinIHfyc5d1cCCxZjDj[YxteyCjdDCwMlMhdWdxbXy= Mn\sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB4MkGxO|UoRjNyNkKxNVc2RC:jPh?=
E9 MUjD[YxtKGe{b4f0bEBie3OjeR?= M3;2[|AtKDBwMTygNE4{KG2pL33s M3PxS|Mh\GG7cx?= NUDOV3E3WE[GIITy[YF1dWWwdDDzbYdvcW[rY3HueIx6KHO3cIDy[ZN{\WRidHjlJIdzd3e2aDDv[kBk\WyuczDheEAxNjNibXevcYw> NIC1R4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|ME[yNVE4PSd-M{C2NlEyPzV:L3G+
F10 NEjGUZBE\WyuIHfyc5d1cCCjc4PhfS=> MXWwMEAxNjFuIECuN{Bu\y:vbB?= MmPtN{Bl[Xm| M3S5VHBHTCC2cnXheI1mdnRic3nncolncWOjboTsfUB{fXCycnXzd4VlKHSqZTDndo94fGhib3[gZ4VtdHNiYYSgNE4{KG2pL33s MkfuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB4MkGxO|UoRjNyNkKxNVc2RC:jPh?=
AIDL NEPKeppE\WyuIHfyc5d1cCCjc4PhfS=> NFfaT3MxNCByLkGsJFAvOyCvZz;tcC=> MVezJIRigXN? MkW0VGZFKHS{ZXH0cYVvfCC|aXfubYZq[2GwdHz5JJN2eHC{ZYPz[YQhfGinIHfyc5d1cCCxZjDj[YxteyCjdDCwMlMhdWdxbXy= NIjWZXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|ME[yNVE4PSd-M{C2NlEyPzV:L3G+
human intestinal fibroblasts (HIFs) MWTGeY5kfGmxbjDhd5NigQ>? NWPhcmxIOSCq M2XyTHBHTCCrbnjpZol1eyCKSV\zJIRq\m[ncnXueIlifGmxbjDhcoQhfGinIHPvcIxi\2WwIHTldI9{cXSrb36gbY5lfWOnZDDifUBVT0ZvzsKxMi=> MmrJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzNUK4OFgoRjNyMUWyPFQ5RC:jPh?=

... 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]
- Collapse
  • Animal Models: Sprague-Dawley rats receiving a low-salt diet
  • Dosages: 250 mg/kg
  • Administration: oral diet
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 37 mg/mL (199.76 mM)
Water Insoluble
Ethanol '37 mg/mL
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 AMR-69
Smiles CC1=CN(C(=O)C=C1)C2=CC=CC=C2

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04607928 Recruiting Drug: Pirfenidone|Drug: Placebo Fibrotic Pulmonary Sequelae Post-COVID19 Infection Institut d''Investigació Biomèdica de Bellvitge August 1 2020 Phase 2
NCT04126538 Recruiting Drug: pirfenidone capsule Renal Insufficiency Beijing Continent Pharmaceutical Co Ltd. August 27 2019 Phase 1
NCT03359863 Active not recruiting Drug: Pirfenidone Restrictive Chronic Lung Allograft Dysfunction|Lung Transplant Rejection University of California San Francisco|Genentech Inc. March 7 2018 Phase 2
NCT02689778 Active not recruiting Drug: Pirfenidone|Drug: Placebo Diabetic Nephropathy|Albuminuria Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran|Grupo Medifarma S. A. de C. V. March 2016 Phase 3
NCT02598193 Completed Drug: Nintedanib|Drug: Pirfenidone Idiopathic Pulmonary Fibrosis Hoffmann-La Roche January 14 2016 Phase 4
NCT02579603 Completed Drug: Nintedanib|Drug: Pirfenidone Idiopathic Pulmonary Fibrosis Boehringer Ingelheim October 16 2015 Phase 4

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