Home TGF-beta/Smad TGF-beta/Smad inhibitor - CCR inhibitor Pirfenidone For research use only.

Pirfenidone

Synonyms: S-7701, AMR-69

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

Pirfenidone Chemical Structure

Pirfenidone Chemical Structure

CAS: 53179-13-8

Selleck's Pirfenidone has been cited by 45 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HFL1 cells Function assay 48 h Antifibrotic activity in HFL1 cells assessed as inhibition of cell viability after 48 hrs by sulforhodamine B assay, IC50 = 0.71 μM. 26896707
LNCaP Cell growth assay 0, 0.1, 0.3 mg/ml 3 days PFD treatment significantly suppressed the growth of cells at 0.3 mg/ml 30621175
PC-3 Cell growth assay 0, 0.1, 0.3 mg/ml 3 days PFD treatment significantly suppressed the growth of cells at 0.3 mg/ml 30621175
E9 Cell growth assay 0, 0.1, 0.3 mg/ml 3 days PFD treatment significantly suppressed the growth of cells at 0.3 mg/ml 30621175
F10 Cell growth assay 0, 0.1, 0.3 mg/ml 3 days PFD treatment significantly suppressed the growth of cells at 0.3 mg/ml 30621175
AIDL Cell growth assay 0, 0.1, 0.3 mg/ml 3 days PFD treatment significantly suppressed the growth of cells at 0.3 mg/ml 30621175
human intestinal fibroblasts (HIFs) Function assay 1 h PFD inhibits HIFs differentiation and the collagen deposition induced by TGF-β1. 30152848
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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. 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
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 Research Cell lines ACHN cells
Concentrations 0.5 mg/ml
Incubation Time 12 h
Method

Cells were treated with various concentrations of drug.
Experimental Result Images Methods Biomarkers Images PMID
Immunofluorescence α-SMA SMAD4 / SMAD2 / SMAD3 F-actin / β-catenin / Vimentin 22132230
In Vivo
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]
Animal Research Animal Models Sprague-Dawley rats receiving a low-salt diet
Dosages 250 mg/kg
Administration oral diet
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05676112 Withdrawn Pulmonary Fibrosis Boehringer Ingelheim|China-Japan Friendship Hospital December 29 2023 --
NCT06070610 Completed Healthy Boehringer Ingelheim November 8 2023 Phase 1
NCT05713292 Active not recruiting COVID-19 Pneumonia Capital Medical University December 30 2022 Phase 3
NCT05505409 Recruiting Pirfenidone|Connective Tissue Diseases|Interstitial Lung Disease Qilu Hospital of Shandong University June 22 2022 Phase 4

Chemical lnformation & Solubility

Molecular Weight 185.22 Formula

C12H11NO
CAS No. 53179-13-8 SDF Download Pirfenidone SDF
Smiles CC1=CN(C(=O)C=C1)C2=CC=CC=C2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 37 mg/mL ( (199.76 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 37 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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