Heparastatin

肝素酶抑制剂；表达重组人酶的A375M人黑色素瘤细胞中的肝素酶（IC50=10.55µM）；抑制牛肝β-葡萄糖醛酸酶和杏仁β-葡萄糖苷酶（IC50s分别为0.31和11µM）；降低角叉菜胶诱发的小鼠背部气囊炎症模型中气囊中性粒细胞和单核细胞浸润以及CCL2水平；每天一次100mg/kg剂量可抑制小鼠Lewis肺癌模型中57.1%的转移。An inhibitor of heparanase; heparanase in A375M human melanoma cells expressing the recombinant human enzyme (IC50 = 10.55 µM); inhibits bovine liver β-glucuronidase and almond β-glucosidase (IC50s = 0.31 and 11 µM, respectively); reduces air pouch neutrophil and monocyte infiltration and CCL2 levels in a carrageenan-induced mouse model of dorsal air pouch inflammation; inhibits metastasis by 57.1% in a murine Lewis lung carcinoma model at 100 mg/kg once per day.分子式C8H11F3N2O5分子量272.2FC(F)(F)C(N[C@@H]1[C@H]([C@H]([C@H](CN1)C(O)=O)O)O)=O