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CAS No. : 182959-33-7
MCE 国际站:YM-53601
产品活性:YM-53601 是一种角鲨烯合酶 (squalene synthase) 抑制剂,可降低体内血浆胆固醇和甘油三酯水平。YM-53601 抑制源自人肝癌细胞的角鲨烯合酶,IC50 为 79 nM。可用作降脂剂。YM-53601 还是法呢基二磷酸法呢基转移酶 1 (FDFT1) 酶活性的抑制剂,可抑制 HCV 传播。
研究领域:Metabolic Enzyme/Protease | Anti-infection
作用靶点:Farnesyl Transferase | HCV
In Vitro: YM-53601 inhibits squalene synthase activities in hepatic microsomes from several species of rat, hamster, guinea-pig, rhesus monkey, and human-derived HepG2 cell with IC50s of 90, 170, 46, 45, and 79 nM, respectively.
YM-53601 inhibits conversion of [3H]farnesyl diphosphate to [3H]squalene by hamster liver squalene synthase with the IC50 of 170 nM.
YM-53601 (1 μM) potentiates the susceptibility of H35 cells to thapsigargin, lonidamine, and doxorubicin. YM-53601 (1 μM) reduces the mitochondrial cholesterol levels in both H35 and HepG2 cells.
In Vivo: YM-53601 suppresses cholesterol biosynthesis in rats (ED50, 32 mg/kg).
YM-53601 also reduces plasma non-HDL cholesterol levels in hamsters by approximately 70% at an oral dose of 50 mg/kg/day for 5 days.
YM-53601 potentiates Doxorubicin-mediated hepatocellular carcinoma cells (HCC) growth arrest and cell death in vivo.
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