Pirfenidone (Synonyms: AMR 69) |
| رقم الكتالوجGC12790 |
Pirfenidone (AMR69) هو عامل مضاد للتليف يعمل على إضعاف إنتاج CCL2 و CCL12 في الخلايا الليفية
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Cas No.: 53179-13-8
Sample solution is provided at 25 µL, 10mM.
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Pirfenidone (AMR69) is an orally active antifibrotic drug that attenuates the production of chemokines CCL2 and CCL12 in fibrocytes[1]. Pirfenidone is a synthetic pyridone drug used to treat idiopathic pulmonary fibrosis (IPF) and also has anti-inflammatory and antioxidant properties [2].
In vitro, pirfenidone (1-10 mM) treatment of human glioma cell lines (LN-18, T98G, LNT-229, and LN-308) for 48 h reduced cell proliferation in a concentration-dependent manner, reduced the levels of the intracellular cytokine transforming growth factor (TGF-β), and reduced the levels of matrix metalloproteinase (MMP-11) [3]. Pirfenidone (2mg/mL) treated intestinal fibroblasts (p-hIFs) for 72 hours reversibly inhibited cell proliferation, inhibited the expression of extracellular matrix proteins (ECM), and inhibited the phosphorylation of the TGF-β1/mTOR/p70S6K signaling pathway mediated by TGF-β1[4].
In vivo, oral treatment of chronic graft-versus-host disease (cGVHD) mice with pirfenidone (400 mg/kg) effectively reduced macrophage infiltration and TGF-β production, and reduced fibrosis and tissue damage in the skin and visceral organs[5]. Oral treatment of idiopathic pulmonary fibrosis (IPF) mice with pirfenidone (300 mg/kg) significantly slowed the progression of pulmonary fibrosis, reduced the mRNA levels of TGF-β, fibronectin and other fibrosis-related genes, and reduced collagen deposition[6].
References:
[1] Inomata M, Kamio K, Azuma A, et al. Pirfenidone inhibits fibrocyte accumulation in the lungs in bleomycin-induced murine pulmonary fibrosis[J]. Respiratory research, 2014, 15: 1-14.
[2] Antar S A, Saleh M A, Al-Karmalawy A A. Investigating the possible mechanisms of pirfenidone to be targeted as a promising anti-inflammatory, anti-fibrotic, anti-oxidant, anti-apoptotic, anti-tumor, and/or anti-SARS-CoV-2[J]. Life Sciences, 2022, 309: 121048.
[3] Burghardt I, Tritschler F, Opitz C A, et al. Pirfenidone inhibits TGF-β expression in malignant glioma cells[J]. Biochemical and biophysical research communications, 2007, 354(2): 542-547.
[4] Cui Y, Zhang M, Leng C, et al. Pirfenidone inhibits cell proliferation and collagen I production of primary human intestinal fibroblasts[J]. Cells, 2020, 9(3): 775.
[5] Du J, Paz K, Flynn R, et al. Pirfenidone ameliorates murine chronic GVHD through inhibition of macrophage infiltration and TGF-β production[J]. Blood, The Journal of the American Society of Hematology, 2017, 129(18): 2570-2580.
[6] Duerr J, Leitz D H W, Szczygiel M, et al. Conditional deletion of Nedd4-2 in lung epithelial cells causes progressive pulmonary fibrosis in adult mice[J]. Nature communications, 2020, 11(1): 2012.
| Cell experiment [1]: | |
|
Cell lines |
LN-18, T98G, LNT-229, LN-308 cells |
|
Preparation Method |
Cells were exposed to Pirfenidone at 1, 2.5, 5 or 10 mM for 48 h. |
|
Reaction Conditions |
1, 2.5, 5 or 10 mM; 48h |
|
Applications |
Pirfenidone caused a concentration-dependent decrease in cell density with IC50 values of 5.5mM (LN-18), 3mM (T98G), 9.5mM (LNT-229), and 9mM (LN-308). |
| Animal experiment [2]: | |
|
Animal models |
Female B10.D2 donor mice and BALB/c recipient mice |
|
Preparation Method |
Pirfenidone crystals were ground down into fine powder using mortar and pestle and then suspended in 0.4% methylcellulose. Mice were given pirfenidone (400 mg/kg) by oral gavage from days 28 to 56 or days 56 to 84 (BO model), days 21 to 55 (B10.D2 to BALB/c model) or days 14 to 27 or 14 to 41 (B6 to B6D2F1 model). |
|
Dosage form |
400mg/kg; p.o. |
|
Applications |
Pirfenidone effectively reduces macrophage infiltration and TGF-β production, leading to an amelioration of chronic graft-versus-host disease (cGVHD) symptoms in a murine model. |
|
References: [1] Burghardt I, Tritschler F, Opitz C A, et al. Pirfenidone inhibits TGF-β expression in malignant glioma cells[J]. Biochemical and biophysical research communications, 2007, 354(2): 542-547. [2]Du J, Paz K, Flynn R, et al. Pirfenidone ameliorates murine chronic GVHD through inhibition of macrophage infiltration and TGF-β production[J]. Blood, The Journal of the American Society of Hematology, 2017, 129(18): 2570-2580. |
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| Cas No. | 53179-13-8 | SDF | |
| المرادفات | AMR 69 | ||
| Chemical Name | 5-methyl-1-phenylpyridin-2-one | ||
| Canonical SMILES | CC1=CN(C(=O)C=C1)C2=CC=CC=C2 | ||
| Formula | C12H11NO | M.Wt | 185.22 |
| الذوبان | ≥ 38.4 mg/mL in DMSO, ≥ 7.68 mg/mL in Water with gentle warming, ≥ 36 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.399 mL | 26.9949 mL | 53.9898 mL |
| 5 mM | 1.0798 mL | 5.399 mL | 10.798 mL |
| 10 mM | 0.5399 mL | 2.6995 mL | 5.399 mL |
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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.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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