1. Stem Cell/Wnt
    TGF-beta/Smad
  2. TGF-beta/Smad

Pirfenidone (Synonyms: AMR69)

Cat. No.: HY-B0673 Purity: 99.84%
Data Sheet SDS Handling Instructions

Pirfenidone leads to a reduction of TGF-β2 mRNA levels and of the mature TGF-β2 protein due to decreased expression and direct inhibition of the TGF-β pro-protein convertase furin.

For research use only. We do not sell to patients.
Pirfenidone Chemical Structure

Pirfenidone Chemical Structure

CAS No. : 53179-13-8

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10 mM * 1 mL in DMSO $66 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Pirfenidone leads to a reduction of TGF-β2 mRNA levels and of the mature TGF-β2 protein due to decreased expression and direct inhibition of the TGF-β pro-protein convertase furin.

IC50 & Target

TGF-β2[1]

In Vitro

Pirfenidone (PFD) reduces the protein levels of the matrix metalloproteinase (MMP)-11, a TGF-β target gene and furin substrate involved in carcinogenesis. These data define PFD or PFD-related agents as promising agents for human cancers associated with enhanced TGF-β activity[1]. In RAW264.7 cells, a murine macrophage-like cell line, Pirfenidone suppresses the proinflammatory cytokine TNF-α by a translational mechanism, which is independent of activation of the MAPK2, p38 MAPK, and JNK. In the murine endotoxin shock model, Pirfenidone potently inhibits the production of the proinflammatory cytokines, TNF-α, interferon-γ, and interleukin-6, but enhances the production of the anti-inflammatory cytokine, interleukin-10[2]. Pirfenidone (PFD) shows its inhibitory effects on the proliferation of HLECs. Cell proliferation is attenuated in the 0.3 mg/mL group after 24 hours compare with the control group (P=0.044). The effect is more apparent in the 0.5 mg/mL group at 24, 48, and 72 hours (P<0.05). The proliferation is almost completely inhibited with 1 mg/mL PFD at all the time-points (P<0.01)[3].

In Vivo

Administration of Pirfenidone (300 mg/kg/day) for 4 wk. Pirfenidone significantly attenuates the score when administered in Bleomycin (BLM)-treated mice (P<0.0001). Moreover, collagen content is quantified in the lungs to evaluate the anti-fibrotic effects of Pirfenidone. The collagen content in the lungs of BLM-treated mice is significantly increased compared with that in saline- or Pirfenidone-treated mice, and this increase is significantly attenuated by Pirfenidone administration on day 28 after BLM treatment (P=0.0012)[4].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02408744 University of Guadalajara|Cell Therapy And Technology, S.a. De C.v. Fibrosis|Chronic Kidney Disease September 2009 Phase 1|Phase 2
NCT03208933 Hoffmann-La Roche Idiopathic Pulmonary Fibrosis June 23, 2017 Phase 3
NCT02598193 Hoffmann-La Roche Idiopathic Pulmonary Fibrosis January 14, 2016 Phase 4
NCT00076102 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Neurofibromatosis 1|Neurofibroma, Plexiform January 2004 Phase 2
NCT02699879 Hoffmann-La Roche Idiopathic Pulmonary Fibrosis February 16, 2012
NCT02262299 Rigshospitalet, Denmark Disorder Related to Lung Transplantation|CLAD, Bronchiolitis Obliterans May 2015 Phase 2|Phase 3
NCT02689778 Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran|Grupo Medifarma, S. A. de C. V. Diabetic Nephropathy|Albuminuria March 2016 Phase 3
NCT02821689 RenJi Hospital Dermatopolymyositis|Interstitial Lung Disease July 2016 Phase 4
NCT02525484 Hoffmann-La Roche Healthy Volunteer August 2015 Phase 1
NCT02932566 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 Cardiac Failure March 7, 2017 Phase 2
NCT02579603 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis October 16, 2015 Phase 4
NCT02808871 Ivan O. Rosas|Brigham and Women's Hospital Rheumatoid Arthritis Interstitial Lung Disease April 7, 2017 Phase 2
NCT03115619 Hoffmann-La Roche Idiopathic Pulmonary Fibrosis April 18, 2017
NCT00001596 William Gahl, M.D.|National Human Genome Research Institute (NHGRI)|National Institutes of Health Clinical Center (CC) Albinism|Inborn Errors of Metabolism|Oculocutaneous Albinism|Platelet Storage Pool Deficiency|Pulmonary Fibrosis September 2005 Phase 2
NCT00080223 Genentech, Inc. Idiopathic Pulmonary Fibrosis|Pulmonary Fibrosis August 31, 2003 Phase 2
NCT01933334 Genentech, Inc. Systemic Sclerosis October 2013 Phase 2
NCT00063583 Sharma, Kumar, M.D.|National Institutes of Health (NIH)|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) Diabetes Mellitus|Diabetic Nephropathy June 2003 Phase 1|Phase 2
NCT02648048 Hoffmann-La Roche Idiopathic Pulmonary Fibrosis January 2016 Phase 1
NCT00662038 Genentech, Inc.|Hoffmann-La Roche Idiopathic Pulmonary Fibrosis August 2008 Phase 3
NCT02951429 Hoffmann-La Roche Idiopathic Pulmonary Fibrosis January 13, 2017 Phase 2
NCT02958917 National Jewish Health|Genentech, Inc. Interstitial Lung Disease March 4, 2017
NCT02161952 University of Guadalajara|Cell Therapy And Technology, S.a. De C.v. Fibrosis|Hepatitis C Chronic May 2005 Phase 2
NCT02136992 Shanghai Pulmonary Hospital, Shanghai, China|Nanjing Chia-tai Tianqing Pharmaceutical Idiopathic Pulmonary Fibrosis December 2011 Phase 2
NCT03099187 Hoffmann-La Roche Lung Diseases, Interstitial May 14, 2017 Phase 2
NCT02622477 Hoffmann-La Roche|InterMune Deutschland GmbH Idiopathic Pulmonary Fibrosis June 2014
NCT03068234 RenJi Hospital Systemic Sclerosis May 2017 Phase 2|Phase 3
NCT00001959 National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) Fibrosis|Focal Glomerulosclerosis|Kidney Failure|Nephrotic Syndrome|Proteinuria December 1999 Phase 2
NCT01504334 Beijing Kawin Technology Share-Holding Co., Ltd. Idiopathic Pulmonary Fibrosis January 2012 Phase 2
NCT02222376 Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran Diabetic Foot Ulcers October 2013 Phase 3
NCT00287729 Genentech, Inc. Idiopathic Pulmonary Fibrosis April 2006 Phase 3
NCT02496182 Grupo Medifarma, S. A. de C. V. Alveolitis Extrinsic Allergic|Pulmonary Fibrosis July 2015 Phase 2|Phase 3
NCT02530359 Hospital Civil de Guadalajara Acute Kidney Injury|Sepsis October 2015 Phase 4
NCT00287716 Genentech, Inc. Idiopathic Pulmonary Fibrosis July 14, 2006 Phase 3
NCT00754780 Mayo Clinic Neurofibromatosis September 2000 Phase 2
NCT01366209 Genentech, Inc. Idiopathic Pulmonary Fibrosis June 2011 Phase 3
NCT02606877 Boehringer Ingelheim Idiopathic Pulmonary Fibrosis April 19, 2016 Phase 4
NCT02632877 University of Guadalajara|Cell Pharma, SA de CV Diabetic Foot Ulcer January 2014 Phase 1|Phase 2
NCT02823236 Centro Dermatológico Dr. Ladislao de la Pascua|Grupo Medifarma, S. A. de C. V. Keloid October 24, 2016 Phase 3
NCT00011076 National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) Hypertrophic Cardiomyopathy February 2001 Phase 2
NCT00020631 National Cancer Institute (NCI) Radiation Fibrosis October 2001
NCT00053937 National Cancer Institute (NCI) Neurofibromatosis Type 1|Precancerous Condition December 2002 Phase 1
NCT03177291 H. Lee Moffitt Cancer Center and Research Institute Lung Cancer|Non Small Cell Lung Cancer|Advanced Cancer|Metastatic Lung Cancer|Squamous Cell Lung Cancer|Non-Squamous Non-Small Cell Neoplasm of Lung October 2017 Phase 1
NCT02141087 Genentech, Inc. Idiopathic Pulmonary Fibrosis
NCT03221257 Michael Roth|University of Michigan|Genentech, Inc.|University of California, Los Angeles Scleroderma, Systemic|Interstitial Lung Disease October 2017 Phase 2
NCT02707640 Hoffmann-La Roche Idiopathic Pulmonary Fibrosis August 2013 Phase 2
NCT02296281 Beijing Continent Pharmaceutical Co, Ltd.|Shanghai Genomics, Inc.|GNI-EPS Pharmaceuticals, Inc. (GNI Group) Radiation Pneumonitis January 2015 Phase 2
NCT00332033 Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|National Institutes of Health Clinical Center (CC) Uterine Leiomyoma|Fibroids May 25, 2006 Phase 2
NCT01872689 Hoffmann-La Roche Idiopathic Pulmonary Fibrosis October 30, 2013 Phase 2
NCT01417156 Boehringer Ingelheim Pulmonary Fibrosis September 2011 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 5.3990 mL 26.9949 mL 53.9898 mL
5 mM 1.0798 mL 5.3990 mL 10.7980 mL
10 mM 0.5399 mL 2.6995 mL 5.3990 mL
Cell Assay
[3]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

Pirfenidone (PFD) is suspended in 0.5% carboxymethylcellulose solution (Mice)[4].

Mice[4]
Nine-week-old female C57BL/6 mice are used. Pirfenidone is administered orally for 14 days after osmotic pump implantation. The volume of administration is determined according to body weight. Animals are allocated into 4 groups (n=6/group): normal control, BLM, Pirfenidone (300 mg/kg/day), and BLM + Pirfenidone. The Pirfenidone dose is selected according to a report published elsewhere. Pirfenidone is also administered in a therapeutic setting beginning at day 10 to assess the effect of the drug on the fibrotic phase of BLM model mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

185.22

Formula

C₁₂H₁₁NO

CAS No.

53179-13-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.84%

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Pirfenidone
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HY-B0673
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