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Purity: ≥98%
Pirfenidone (formerly AMR69; S7701, AMR-69; S-7701; trade name: Pirespa; Pirfenex; Deskar, Esbriet) is a potent inhibitor for TGF-β production and TGF-β stimulated collagen production with anti-fibrotic and anti-inflammatory properties. It has been used as a medication for the treatment of idiopathic pulmonary fibrosis. It reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. 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.
| ln Vitro |
The furin substrate matrix metalloproteinase (MMP)-11, a TGF-β target gene implicated in carcinogenesis, had its protein levels decreased by pirfenidone (PFD). According to these findings, PFD or PFD-related medicines are prospective treatments for human malignancies linked to increased TGF-β activity[1]. Through a translational mechanism, pirfenidone inhibits the proinflammatory cytokine TNF-α in RAW264.7 cells, a murine macrophage-like cell line, without requiring activation of MAPK2, p38 MAPK, or JNK. Pirfenidone significantly reduces the synthesis of proinflammatory cytokines such as TNF-α, interferon-γ, and interleukin-6 in the murine endotoxin shock model, while increasing the synthesis of interleukin-10, an anti-inflammatory cytokine[2]. PFD (pirfenidone) exhibits its inhibitory effects on HLEC growth. After 24 hours, there is a reduction in cell growth in the 0.3 mg/mL group compared to the control group (P=0.044). At 24, 48, and 72 hours, the impact is more noticeable in the 0.5 mg/mL group (P<0.05). At all time points, 1 mg/mL PFD virtually entirely inhibits growth (P<0.01)[3].
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| ln Vivo |
Pirfenidone (300 mg/kg/day) was administered for four weeks. When pirfenidone is given to mice treated with Bleomycin (BLM), the score is dramatically reduced (P<0.0001). In addition, lung collagen content is measured in order to assess Pirfenidone's anti-fibrotic properties. When compared to mice treated with saline or pirfenidone, the lungs of BLM-treated mice have a significantly higher collagen content, and this rise is dramatically reduced when pirfenidone is administered on day 28 following BLM treatment (P=0.0012)[4].
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| References |
[1]. Burghardt I, et al. Pirfenidone inhibits TGF-beta expression in malignant glioma cells. Biochem Biophys Res Commun. 2007 Mar 9;354(2):542-7.
[2]. Nakazato H, et al. A novel anti-fibrotic agent pirfenidone suppresses tumor necrosis factor-alpha at the translational level. Eur J Pharmacol. 2002 Jun 20;446(1-3):177-85. [3]. Yang Y, et al. Inhibition of Pirfenidone on TGF-beta2 induced proliferation, migration and epithlial-mesenchymal transitionof human lens epithelial cells line SRA01/04. PLoS One. 2013;8(2):e56837. [4]. Inomata M, et al. Pirfenidone inhibits fibrocyte accumulation in the lungs in bleomycin-induced murine pulmonary fibrosis. Respir Res. 2014 Feb 8;15:16. [5]. Brooks D, et al. Limited fibrosis accompanies triple-negative breast cancer metastasis in multiple model systems and is not a preventive target. Oncotarget. 2018 May 4;9(34):23462-23481 |
| Molecular Formula |
C12H11NO
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| Molecular Weight |
185.22
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| CAS # |
53179-13-8
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| SMILES |
O=C1C([H])=C([H])C(C([H])([H])[H])=C([H])N1C1C([H])=C([H])C([H])=C([H])C=1[H]
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| Synonyms |
S-7701, AMR-69; S 7701, AMR69; S7701, AMR-69; AMR 69; Pirfenidone; trade name: Pirespa; Pirfenex; Deskar, Esbriet; Etuary.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (14.85 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (14.85 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (11.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (11.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 2.08 mg/mL (11.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 6: 2% DMSO+30% PEG 300+ddH2O:10 mg/mL Solubility in Formulation 7: 9.09 mg/mL (49.08 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). Solubility in Formulation 8: 6.67 mg/mL (36.01 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 9: 20 mg/mL (107.98 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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