Pirfenidone (S-7701)

Catalog No.S2907 Synonyms: AMR-69

For research use only.

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.

Pirfenidone (S-7701) Chemical Structure

CAS No. 53179-13-8

Selleck's Pirfenidone (S-7701) has been cited by 37 publications

Purity & Quality Control

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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 M4rZNGZ2dmO2aX;uJIF{e2G7 NGHYUZI1QCCq M2TLVGFvfGmoaXLyc5Rq[yCjY4Tpeol1gSCrbjDISmwyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGlEPTBiPTCwMlcyKM7:TT6= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh7NkewO{c,OjZ6OU[3NFc9N2F-
LNCaP NEi2WVJE\WyuIHfyc5d1cCCjc4PhfS=> NGXFT4gxNCByLkGsJFAvOyCvZz;tcC=> NXnjVY52OyCmYYnz MWTQSmQhfHKnYYTt[Y51KHOrZ37p[olk[W62bImgd5VxeHKnc4Pl[EB1cGViZ4Lve5RpKG:oIHPlcIx{KGG2IECuN{Bu\y:vbB?= M2C5UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNkKxNVc2Lz5|ME[yNVE4PTxxYU6=
PC-3 M4TVO2NmdGxiZ4Lve5RpKGG|c3H5 Mm[2NEwhOC5zLDCwMlMhdWdxbXy= NVjpU3FPOyCmYYnz MUPQSmQhfHKnYYTt[Y51KHOrZ37p[olk[W62bImgd5VxeHKnc4Pl[EB1cGViZ4Lve5RpKG:oIHPlcIx{KGG2IECuN{Bu\y:vbB?= M17hclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNkKxNVc2Lz5|ME[yNVE4PTxxYU6=
E9 M1:3ZmNmdGxiZ4Lve5RpKGG|c3H5 M4niO|AtKDBwMTygNE4{KG2pL33s M165dFMh\GG7cx?= NVftToFQWE[GIITy[YF1dWWwdDDzbYdvcW[rY3HueIx6KHO3cIDy[ZN{\WRidHjlJIdzd3e2aDDv[kBk\WyuczDheEAxNjNibXevcYw> MnfEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB4MkGxO|UoRjNyNkKxNVc2RC:jPh?=
F10 NITyXXpE\WyuIHfyc5d1cCCjc4PhfS=> MVmwMEAxNjFuIECuN{Bu\y:vbB?= MnrIN{Bl[Xm| M{n5[HBHTCC2cnXheI1mdnRic3nncolncWOjboTsfUB{fXCycnXzd4VlKHSqZTDndo94fGhib3[gZ4VtdHNiYYSgNE4{KG2pL33s MkizQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB4MkGxO|UoRjNyNkKxNVc2RC:jPh?=
AIDL MkL6R4VtdCCpcn;3eIgh[XO|YYm= MX2wMEAxNjFuIECuN{Bu\y:vbB?= MnruN{Bl[Xm| NXzoSIozWE[GIITy[YF1dWWwdDDzbYdvcW[rY3HueIx6KHO3cIDy[ZN{\WRidHjlJIdzd3e2aDDv[kBk\WyuczDheEAxNjNibXevcYw> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODZ{MUG3OUc,OzB4MkGxO|U9N2F-
human intestinal fibroblasts (HIFs) M1zMRWZ2dmO2aX;uJIF{e2G7 Mkn2NUBp Ml7HVGZFKGmwaHnibZR{KEiLRoOg[Iln\mW{ZX70bYF1cW:wIHHu[EB1cGViY3;scIFo\W5iZHXwc5NqfGmxbjDpcoR2[2WmIHL5JHRITi4QskGu MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODF3Mki0PEc,OzBzNUK4OFg9N2F-
Assay
Methods Test Index PMID
Immunofluorescence α-SMA ; SMAD4 / SMAD2 / SMAD3 ; F-actin / β-catenin / Vimentin 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 (from reference)

Animal Research:[3]
  • Animal Models: Sprague-Dawley rats receiving a low-salt diet
  • Dosages: 250 mg/kg
  • Administration: oral diet

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 185.22
Formula

C12H11NO

CAS No. 53179-13-8
Storage 3 years -20°C powder
2 years -80°C in solvent
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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Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04971746 Completed Drug: Pirfenidone|Drug: GLPG4716|Drug: Nintedanib Healthy Galapagos NV July 19 2021 Phase 1
NCT04888715 Completed Drug: DWN12088|Drug: Pirfenidone|Drug: Nintedanib Idiopathic Pulmonary Fibrosis Daewoong Pharmaceutical Co. LTD. July 23 2021 Phase 1
NCT05383131 Completed Drug: HEC585|Drug: Pirfenidone|Drug: Nintedanib Idiopathic Pulmonary Fibrosis Sunshine Lake Pharma Co. Ltd. June 23 2021 Phase 1
NCT05060822 Recruiting Drug: HEC585|Drug: Pirfenidone|Drug: Placebo Idiopathic Pulmonary Fibrosis Sunshine Lake Pharma Co. Ltd. June 30 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

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