Pirfenidone
(Synonyms: 吡非尼酮; AMR69) 目录号 : GC12790
吡非尼酮（Pirfenidone；AMR69）是一种具有口服活性的抗纤维化药物，可减弱纤维细胞中趋化因子CCL2和CCL12的产生。
Cas No.:53179-13-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
LN-18, T98G, LNT-229, LN-308 cells |
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Preparation Method |
Cells were exposed to Pirfenidone at 1, 2.5, 5 or 10 mM for 48 h. |
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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]: | |
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Animal models |
Female B10.D2 donor mice and BALB/c recipient mice |
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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). |
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Dosage form |
400mg/kg; p.o. |
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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. |
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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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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.
吡非尼酮（Pirfenidone；AMR69）是一种具有口服活性的抗纤维化药物，可减弱纤维细胞中趋化因子CCL2和CCL12的产生[1]。Pirfenidone是一种合成吡啶酮药物，用于治疗特发性肺纤维化（IPF），还具有抗炎和抗氧化特性[2]。
在体外，Pirfenidone（1-10 mM）处理人神经胶质瘤细胞系（LN-18、T98G、LNT-229和LN-308）48h，浓度依赖性地降低了细胞增殖，降低了胞内细胞因子转化生长因子（TGF-β）的水平，还降低了基质金属蛋白酶（MMP-11）的水平[3]。Pirfenidone（2mg/mL）处理肠道成纤维细胞（p-hIFs）72h，可逆地抑制细胞的增殖，抑制细胞外基质蛋白（ECM）的表达，抑制TGF-β1介导的 TGF-β1/mTOR/p70S6K信号通路的磷酸化[4]。
在体内，Pirfenidone（400mg/kg）通过口服治疗慢性移植物抗宿主病（cGVHD）小鼠，有效减少巨噬细胞浸润和TGF-β的产生，减少皮肤和内脏器官纤维化和组织损伤[5]。Pirfenidone（300mg/kg）通过口服治疗特发性肺纤维化（IPF）小鼠，显著减缓了肺纤维化的进展，降低了TGF-β、纤连蛋白和其他纤维化相关基因的 mRNA水平，减少了胶原蛋白沉积[6]。
| Cas No. | 53179-13-8 | SDF | |
| 别名 | 吡非尼酮; AMR69 | ||
| 化学名 | 5-methyl-1-phenylpyridin-2-one | ||
| Canonical SMILES | CC1=CN(C(=O)C=C1)C2=CC=CC=C2 | ||
| 分子式 | C12H11NO | 分子量 | 185.22 |
| 溶解度 | ≥ 38.4 mg/mL in DMSO, ≥ 7.68 mg/mL in Water with gentle warming, ≥ 36 mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。