Pirfenidone

製品コードS2907 バッチS290704

化学情報

	Synonyms	S-7701, AMR-69	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₂H₁₁NO
	分子量	185.22	CAS No.	53179-13-8
Solubility (25°C)*	体外	DMSO	37 mg/mL (199.76 mM)
		Ethanol	37 mg/mL (199.76 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Pirfenidone 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.
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]
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]

製品説明

Pirfenidone 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.

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]

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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	ACHN cells
	濃度	0.5 mg/ml
	反応時間	12 h
	実験の流れ	Cells were treated with various concentrations of drug.
動物実験	動物モデル	Sprague-Dawley rats receiving a low-salt diet
	投薬量	250 mg/kg
	投与方法	oral diet

参考

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カスタマーフィードバック

: Data from [Data independently produced by Histochem Cell Biol, 2014, 142(4), 361-71]

: , , Am J Respir Cell Mol Biol, 2017, 57(1):77-90

: Data from [Data independently produced by , , Aging Cell, 2018, doi: 10.1111/acel.12788]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Repositioning of ezetimibe for the treatment of idiopathic pulmonary fibrosis [ Eur Respir J, 2024, 2300580]	PubMed: 38359963
Modulation of Extracellular Matrix Composition and Chronic Inflammation with Pirfenidone Promotes Scar Reduction in Retinal Wound Repair [ Cells, 2024, 13(2)164]	PubMed: 38247855
Fisetin ameliorates fibrotic kidney disease in mice via inhibiting ACSL4-mediated tubular ferroptosis [ Acta Pharmacol Sin, 2023, 10.1038/s41401-023-01156-w]	PubMed: 37696989
Macrophage activity at the site of tumor ablation can promote murine urothelial cancer via transforming growth factor-β1 [ Front Immunol, 2023, 14:1070196]	PubMed: 36761730
Differences in Treatment Response in Bronchial Epithelial Cells from Idiopathic Pulmonary Fibrosis (IPF) Patients: A First Step towards Personalized Medicine [ Antioxidants (Basel), 2023, 12(2)443]	PubMed: 36830000
Differences in Treatment Response in Bronchial Epithelial Cells from Idiopathic Pulmonary Fibrosis -IPF) Patients: A First Step towards Personalized Medicine [ Antioxidants -Basel), 2023, 12(2)443]	PubMed: 36830000
Impact of in vitro HIV infection on human thymic regulatory T cell differentiation [ Front Microbiol, 2023, 14:1217801]	PubMed: 37547675
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7]	PubMed: 34997030
The Anti-fibrosis drug Pirfenidone modifies the immunosuppressive tumor microenvironment and prevents the progression of renal cell carcinoma by inhibiting tumor autocrine TGF-β [ Cancer Biol Ther, 2022, 23(1):150-162]	PubMed: 35130111
Contracting scars from fibrin drops [ Integr Biol (Camb), 2022, 14(1):1-12]	PubMed: 35184163

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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