GED-0507-34 Levo ((S)-3-(4-Aminophenyl)-2-methoxypropanoic acid), an orally available PPARγ modulator for amelioration of inflammation-driven intestinal fibrosis, decreased the expression of the pro-fibrotic genes Acta2, COL1a1, and Fn1, reduced the protein levels of α-SMA and collagen I-II, the main markers of fibrosis, as well as the major components of the TGFβ/Smad pathway, and decreased the expression of IL-13, CTGF, TGFB and ACTA1, and inhibited TGF-β-induced activation of fibroblasts and IECs cell lines.

在 TGF-β 刺激的肠道成纤维细胞、上皮细胞系及溃疡性结肠炎患者来源的原代成纤维细胞中加入 GED-0507-34 Levo，检测 α-SMA、Fn1、TGF-β、ACTA1 等的表达及表型变化。结果表明 GED 抑制了 TGF-β 诱导的细胞活化过程[1]。

C57BL/6 小鼠（n = 110）通过 2.5% DSS（饮水，3轮，6周）诱导肠道纤维化，同时每日口服给予 GED-0507-34 Levo（30 mg/kg/d）。通过宏观与组织学评分及纤维化相关基因/蛋白检测评估疗效。结果显示 GED 可减轻小鼠肠道纤维化[1]。