Pirfenidone吡非尼酮,53179-13-8

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Pirfenidone

CAS No. : 53179-13-8

MCE 国际站：Pirfenidone

产品活性：Pirfenidone (AMR69) 是一种抗纤维化剂，可减弱纤维细胞中 CCL2 和 CCL12 的产生。Pirfenidone 具有抑制细胞生长的作用，并能降低人胶质瘤细胞系中的 TGF-β2 蛋白水平。Pirfenidone 还具有抗炎活性。

研究领域：Stem Cell/Wnt  |  TGF-beta/Smad  |  GPCR/G Protein  |  Immunology/Inflammation

作用靶点：TGF-beta/Smad  |  CCR

In Vitro: Pirfenidone (PFD) reduces the protein levels of the matrix metalloproteinase (MMP)-11, a TGF-β target gene and furin substrate involved in carcinogenesis. These data define PFD or PFD-related agents as promising agents for human cancers associated with enhanced TGF-β activity. In RAW264.7 cells, a murine macrophage-like cell line, Pirfenidone suppresses the proinflammatory cytokine TNF-α by a translational mechanism, which is independent of activation of the MAPK2, p38 MAPK, and JNK. In the murine endotoxin shock model, Pirfenidone potently inhibits the production of the proinflammatory cytokines, TNF-α, interferon-γ, and interleukin-6, but enhances the production of the anti-inflammatory cytokine, interleukin-10. Pirfenidone (PFD) shows its inhibitory effects on the proliferation of HLECs. Cell proliferation is attenuated in the 0.3 mg/mL group after 24 hours compare with the control group (P=0.044). The effect is more apparent in the 0.5 mg/mL group at 24, 48, and 72 hours (P<0.05). The proliferation is almost completely inhibited with 1 mg/mL PFD at all the time-points (P<0.01).

In Vivo: Administration of Pirfenidone (300 mg/kg/day) for 4 wk. Pirfenidone significantly attenuates the score when administered in Bleomycin (BLM)-treated mice (P<0.0001). Moreover, collagen content is quantified in the lungs to evaluate the anti-fibrotic effects of Pirfenidone. The collagen content in the lungs of BLM-treated mice is significantly increased compared with that in saline- or Pirfenidone-treated mice, and this increase is significantly attenuated by Pirfenidone administration on day 28 after BLM treatment (P=0.0012).

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