| CAS NO: | 53179-13-8 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| Molecular Weight (MW) | 185.22 |
|---|---|
| Formula | C12H11NO |
| CAS No. | 53179-13-8 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 37 mg/mL (199.8 mM) |
| Water: <1 mg/mL | |
| Ethanol: 37 mg/mL (199.8 mM) | |
| Solubility (In vivo) | 2% DMSO+30% PEG 300+ddH2O: 10 mg/mL |
| Synonyms | S-7701, AMR-69; S 7701, AMR69; S7701, AMR-69; AMR 69; Pirfenidone; trade name: Pirespa; Pirfenex; Deskar, Esbriet; Etuary. |
| In Vitro | In vitro activity: 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). 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. Kinase Assay: Cell Assay: In RAW264.7 cells, Pirfenidone (< 300 μg/mL) suppressed the proinflammatory cytokine tumor necrosis factor-α (TNF-α) through a translational mechanism, which was independent of activation of the mitogen-activated protein kinase (MAPK)2, p38 MAP kinase, and c-Jun N-terminal kinase (JNK). In LN-18, T98G, LNT-229 and LN-308 cell lines, Pirfenidone (< 10 mM) reduced glioma cell density in a concentration-dependent manner. In CCL-64 cells, Pirfenidone (< 5 mM) reduced TGF-β bioactivity by affecting TGF-β2 mRNA expression and processing of pro-TGF-β. Pirfenidone (< 8.3 mM) inhibited the activity of recombinant furin and downregulated the expression of MMP-11 in a dose-dependent manner in LN-308 cells. In cultured myometrial and leiomyoma smooth muscle cells, pirfenidone inhibited serum-stimulated increases in DNA synthesis and cell proliferation in a dose-dependent manner. |
|---|---|
| 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. 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. 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. 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. |
| Animal model | Sprague-Dawley rats receiving a low-salt diet |
| Formulation & Dosage | Dissolved in saline; 250 mg/kg; oral gavage |
| References | Eur J Pharmacol. 2002 Jun 20;446(1-3):177-85; Am J Transplant. 2002 Feb;2(2):111-9. |
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