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MedKoo Cat#: 317114 | Name: Pirfenidone
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pirfenidone is an anti-fibrotic drug for the treatment of idiopathic pulmonary fibrosis (IPF). It works by reducing lung fibrosis through downregulation of the production of growth factors and procollagens I and II. Pirfenidone has well-established antifibrotic and anti-inflammatory properties in various in vitro systems and animal models of fibrosis. A number of cell-based studies have shown that pirfenidone reduces fibroblast proliferation, inhibits TGF-β stimulated collagen production and reduces the production of fibrogenic mediators such as TGF-β.

Chemical Structure

Pirfenidone
Pirfenidone
CAS#53179-13-8

Theoretical Analysis

MedKoo Cat#: 317114

Name: Pirfenidone

CAS#: 53179-13-8

Chemical Formula: C12H11NO

Exact Mass: 185.0841

Molecular Weight: 185.22

Elemental Analysis: C, 77.81; H, 5.99; N, 7.56; O, 8.64

Price and Availability

Size Price Availability Quantity
500mg USD 150.00 Ready to ship
1g USD 220.00 Ready to ship
2g USD 325.00 Ready to ship
5g USD 550.00 Ready to ship
10g USD 850.00 Ready to ship
25g USD 1,650.00 Ready to ship
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Related CAS #
No Data
Synonym
AMR69; AMR-69; AMR 69; Pirfenidone; brand name: Pirespa; Pirfenex; Deskar, Esbriet; Etuary.
IUPAC/Chemical Name
5-methyl-1-phenyl-2-(1H)-pyridone
InChi Key
ISWRGOKTTBVCFA-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H11NO/c1-10-7-8-12(14)13(9-10)11-5-3-2-4-6-11/h2-9H,1H3
SMILES Code
O=C1C=CC(C)=CN1C2=CC=CC=C2
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells.
In vitro activity:
A CCK8 cell proliferation assay was performed to determine the influence of PFD (Pirfenidone) and TGF-β1 on FLSs (fibroblast-like synoviocytes). The results indicate that PFD inhibited the proliferation of FLSs, the degree of inhibition essentially dose-dependent at 24 h, 48 h, and 72 h (Fig. 1a). The maximum inhibition was observed at 2.0 mg/ml after 48 h. TGF-β1 facilitated FLS proliferation, the rate reaching a plateau at a concentration of 2.5 ng/ml (Fig. 1b). Therefore, 2.5 ng/ml TGF-β1 was used for subsequent FLS experiments, including analysis using Transwell assays, real-time quantitive PCR, and ELISA. Reference: J Transl Med. 2021; 19: 157. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8054406/
In vivo activity:
Compared to the normal group, CIA (collagen-induced arthritis) rats had greater hindfoot paw thickness, and both MTX and PFD (Pirfenidone) treatments reduced hindfoot swelling (p < 0.05) (Figures 1B,F). As determined with an ultrasound analysis, synovial thickness of the knee joint was significantly lower in the CIA rats treated with PFD than in the untreated CIA rats (p < 0.05) (Figures 1C,F). H&E staining showed that, compared with the CIA group, PFD significantly alleviated synovial hyperplasia and inflammatory cell infiltration in the knee joints (p < 0.05) (Figures 1D,F); immunohistochemistry also indicated that PFD effectively reduced VEGF protein expression in CIA joints (Figure 1E). Reference: Front Pharmacol. 2021; 12: 631891. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7973213/
Solvent mg/mL mM comments
Solubility
DMSO 15.0 81.00
Ethanol 20.0 108.00
Water 3.7 20.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 185.22 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Wei Q, Kong N, Liu X, Tian R, Jiao M, Li Y, Guan H, Wang K, Yang P. Pirfenidone attenuates synovial fibrosis and postpones the progression of osteoarthritis by anti-fibrotic and anti-inflammatory properties in vivo and in vitro. J Transl Med. 2021 Apr 19;19(1):157. doi: 10.1186/s12967-021-02823-4. PMID: 33874948; PMCID: PMC8054406. 2. Fujiwara A, Funaki S, Fukui E, Kimura K, Kanou T, Ose N, Minami M, Shintani Y. Effects of pirfenidone targeting the tumor microenvironment and tumor-stroma interaction as a novel treatment for non-small cell lung cancer. Sci Rep. 2020 Jul 2;10(1):10900. doi: 10.1038/s41598-020-67904-8. PMID: 32616870; PMCID: PMC7331721. 3. Gan D, Cheng W, Ke L, Sun AR, Jia Q, Chen J, Lin J, Li J, Xu Z, Zhang P. Repurposing of Pirfenidone (Anti-Pulmonary Fibrosis Drug) for Treatment of Rheumatoid Arthritis. Front Pharmacol. 2021 Mar 5;12:631891. doi: 10.3389/fphar.2021.631891. PMID: 33746759; PMCID: PMC7973213. 4. Lv Q, Wang J, Xu C, Huang X, Ruan Z, Dai Y. Pirfenidone alleviates pulmonary fibrosis in vitro and in vivo through regulating Wnt/GSK-3β/β-catenin and TGF-β1/Smad2/3 signaling pathways. Mol Med. 2020 May 24;26(1):49. doi: 10.1186/s10020-020-00173-3. PMID: 32448163; PMCID: PMC7245944.
In vitro protocol:
1. Wei Q, Kong N, Liu X, Tian R, Jiao M, Li Y, Guan H, Wang K, Yang P. Pirfenidone attenuates synovial fibrosis and postpones the progression of osteoarthritis by anti-fibrotic and anti-inflammatory properties in vivo and in vitro. J Transl Med. 2021 Apr 19;19(1):157. doi: 10.1186/s12967-021-02823-4. PMID: 33874948; PMCID: PMC8054406. 2. Fujiwara A, Funaki S, Fukui E, Kimura K, Kanou T, Ose N, Minami M, Shintani Y. Effects of pirfenidone targeting the tumor microenvironment and tumor-stroma interaction as a novel treatment for non-small cell lung cancer. Sci Rep. 2020 Jul 2;10(1):10900. doi: 10.1038/s41598-020-67904-8. PMID: 32616870; PMCID: PMC7331721.
In vivo protocol:
1. Gan D, Cheng W, Ke L, Sun AR, Jia Q, Chen J, Lin J, Li J, Xu Z, Zhang P. Repurposing of Pirfenidone (Anti-Pulmonary Fibrosis Drug) for Treatment of Rheumatoid Arthritis. Front Pharmacol. 2021 Mar 5;12:631891. doi: 10.3389/fphar.2021.631891. PMID: 33746759; PMCID: PMC7973213. 2. Lv Q, Wang J, Xu C, Huang X, Ruan Z, Dai Y. Pirfenidone alleviates pulmonary fibrosis in vitro and in vivo through regulating Wnt/GSK-3β/β-catenin and TGF-β1/Smad2/3 signaling pathways. Mol Med. 2020 May 24;26(1):49. doi: 10.1186/s10020-020-00173-3. PMID: 32448163; PMCID: PMC7245944.
1: Kang J, Lee KH, Lee JH, Jeong YY, Choi SM, Kim HC, Park JH, Lee HK, Yong SJ, Choi HS, Kim HR, Jegal Y, Choi WI, Lee EJ, Song JW. Safety, effectiveness, and usefulness of higher-dose tablets of generic pirfenidone in patients with IPF: a nationwide observational study in South Korea. Front Pharmacol. 2024 Aug 9;15:1451447. doi: 10.3389/fphar.2024.1451447. PMID: 39185314; PMCID: PMC11341391. 2: Bai Y, Liu F, Luo S, Wan Y, Zhang L, Wu X, Chen Q, Xie Y, Guo P. Experimental study on H2O2 activation of HSC-T6 and hepatic fibrosis in cholestatic mice by "Yajieshaba". J Ethnopharmacol. 2024 Aug 22;335:118712. doi: 10.1016/j.jep.2024.118712. Epub ahead of print. PMID: 39173724. 3: Han M, Liu Q, Ji Z, Jin L, Jin W, Gao Z. Use of pirfenidone in fibrotic interstitial lung diseases and beyond: a review. Front Med (Lausanne). 2024 Aug 6;11:1411279. doi: 10.3389/fmed.2024.1411279. PMID: 39165369; PMCID: PMC11333372. 4: Yıldırım AB, Göl M, Yiğin A, Çimen L, Dinç H, Yıldız H, Kayar B. Therapeutic use of fisetin and pirfenidone combination in bleomycin-induced pulmonary fibrosis in adult male albino rats. Naunyn Schmiedebergs Arch Pharmacol. 2024 Aug 20. doi: 10.1007/s00210-024-03363-6. Epub ahead of print. PMID: 39162796. 5: Luo X, Xiang F. Acute exacerbation of idiopathic pulmonary fibrosis a narrative review primary focus on treatments. J Thorac Dis. 2024 Jul 30;16(7):4727-4741. doi: 10.21037/jtd-23-1565. Epub 2024 Jul 11. PMID: 39144320; PMCID: PMC11320219. 6: Yu Y, Xu Y, Chen J, Yao Y, Liu Y, Chen Y, Yang B, Guo Z. Pirfenidone improves early cardiac function following myocardial infarction by enhancing the elastin/collagen ratio. Biomed Pharmacother. 2024 Sep;178:117254. doi: 10.1016/j.biopha.2024.117254. Epub 2024 Aug 13. PMID: 39142250. 7: Im CY, Kim SH, Song KH, Ryu MO, Youn HY, Seo KW. Pirfenidone inhibits TGF-β1-induced fibrosis via downregulation of Smad and ERK pathway in MDCK cells. Vet Res Commun. 2024 Aug 12. doi: 10.1007/s11259-024-10493-y. Epub ahead of print. PMID: 39133399. 8: Ma L, Yin L, Zhu H, Li J, Wang D. Two-dimensional vascularized liver organoid on extracellular matrix with defined stiffness for modeling fibrotic and normal tissues. J Tissue Eng. 2024 Aug 10;15:20417314241268344. doi: 10.1177/20417314241268344. PMID: 39130682; PMCID: PMC11316963. 9: Paik SS, Lee JM, Ko IG, Kim SR, Kang SW, An J, Kim JA, Kim D, Hwang L, Jin JJ, Kim SH, Cha JY, Choi CW. Pirfenidone Alleviates Inflammation and Fibrosis of Acute Respiratory Distress Syndrome by Modulating the Transforming Growth Factor-β/Smad Signaling Pathway. Int J Mol Sci. 2024 Jul 23;25(15):8014. doi: 10.3390/ijms25158014. PMID: 39125585; PMCID: PMC11311955. 10: Cottin V, Valenzuela C. Evidence from recent clinical trials in fibrotic interstitial lung diseases. Curr Opin Pulm Med. 2024 Sep 1;30(5):484-493. doi: 10.1097/MCP.0000000000001089. Epub 2024 Jul 4. PMID: 39114938. 11: Lei Y, Sheng JH, Jin XR, Liu XB, Zheng XY, Xu XH. Study on the efficacy of early treatment with pirfenidone on the lung function of patients with idiopathic pulmonary fibrosis. World J Clin Cases. 2024 Aug 6;12(22):4913-4923. doi: 10.12998/wjcc.v12.i22.4913. PMID: 39109030; PMCID: PMC11238781. 12: Fan ZK, Niu XY, Wang LD, Niu YY, Wang LJ, Wang X, Wu YQ, Zhang RT. [Effect of Peitu Yifei Granules on autophagy mechanism in rats with idiopathic pulmonary fibrosis based on PI3K/Akt/mTOR signaling pathway]. Zhongguo Zhong Yao Za Zhi. 2024 Jul;49(14):3878-3886. Chinese. doi: 10.19540/j.cnki.cjcmm.20240321.701. PMID: 39099361. 13: Xu J, Zhou L, Chen H, He Y, Zhao G, Li L, Efferth T, Ding Z, Shan L. Aerosol inhalation of total ginsenosides repairs acute lung injury and inhibits pulmonary fibrosis through SMAD2 signaling-mediated mechanism. Phytomedicine. 2024 Jul 14;133:155871. doi: 10.1016/j.phymed.2024.155871. Epub ahead of print. PMID: 39098168. 14: Chong WH, Agrawal D, Tan ZY, Venkateswaran S, Tan AYY, Tan CY, Ling NCA, Tay NSWT. A systematic review and meta-analysis of the clinical benefits and adverse reactions of anti-fibrotics in non-IPF progressive fibrosing ILD. Heart Lung. 2024 Jul 31;68:242-253. doi: 10.1016/j.hrtlng.2024.07.010. Epub ahead of print. PMID: 39089077. 15: Hozumi H, Miyashita K, Nakatani E, Inoue Y, Yasui H, Suzuki Y, Karayama M, Furuhashi K, Enomoto N, Fujisawa T, Inui N, Suda T. Antifibrotics and mortality in idiopathic pulmonary fibrosis: external validity and avoidance of immortal time bias. Respir Res. 2024 Jul 31;25(1):293. doi: 10.1186/s12931-024-02922-y. PMID: 39085869; PMCID: PMC11293013. 16: Behera AK, Kumar V, Sharma P, Ganga R, Meher J, Pati S, Sinha K. Antifibrotics in the Management of Rheumatoid Arthritis-Associated Interstitial Lung Disease: Prospective Real-World Experience From an Interstitial Lung Disease Clinic in India. Cureus. 2024 Jun 30;16(6):e63518. doi: 10.7759/cureus.63518. PMID: 39081417; PMCID: PMC11288335. 17: Ziaastani Z, Kalantari-Khandani B, Niazi MJ, Kazemipour A. Identification of critical genes and metabolic pathways in rheumatoid arthritis and osteoporosis toward drug repurposing. Comput Biol Med. 2024 Jul 29;180:108912. doi: 10.1016/j.compbiomed.2024.108912. Epub ahead of print. PMID: 39079412. 18: Kreuter M, Lee JS, Tzouvelekis A, Oldham JM, Molyneaux PL, Weycker D, Atwood M, Samara K, Kirchgässler KU, Maher TM. Modified blood cell GAP model as a prognostic biomarker in idiopathic pulmonary fibrosis. ERJ Open Res. 2024 Jul 29;10(4):00666-2023. doi: 10.1183/23120541.00666-2023. PMID: 39076530; PMCID: PMC11284599. 19: Kulkarni T, Newton CA, Gupta S, Samara K, Bernstein EJ. The Impact of Autoantibodies on Outcomes in Patients with Idiopathic Pulmonary Fibrosis: Post- Hoc Analyses of the Phase III ASCEND Trial. Pulm Ther. 2024 Sep;10(3):331-346. doi: 10.1007/s41030-024-00267-x. Epub 2024 Jul 29. PMID: 39073523; PMCID: PMC11339214. 20: Reccardini N, Chernovsky M, Salton F, Confalonieri P, Mondini L, Barbieri M, Romallo A, Maggisano M, Torregiani C, Geri P, Hughes M, Campochiaro C, Confalonieri M, Scarda A, Zuccon U, Ruaro B. Pirfenidone in Idiopathic Pulmonary Fibrosis: Real-World Observation on Efficacy and Safety, Focus on Patients Undergoing Antithrombotic and Anticoagulant. Pharmaceuticals (Basel). 2024 Jul 11;17(7):930. doi: 10.3390/ph17070930. PMID: 39065780; PMCID: PMC11280355.