YM-53601,182959-28-0

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YM-53601 free base

CAS No. : 182959-28-0

MCE 国际站：YM-53601 free base

产品活性：YM-53601 free base 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 free base 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 free base 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 free base 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 free base inhibits conversion of [3H]farnesyl diphosphate to [³H]squalene by hamster liver squalene synthase with the IC₅₀ of 170 nM.
YM-53601 (1 μM) free base potentiates the susceptibility of H35 cells to thapsigargin, lonidamine, and doxorubicin. YM-53601 (1 μM) free base reduces the mitochondrial cholesterol levels in both H35 and HepG2 cells.

In Vivo: YM-53601 free base suppresses cholesterol biosynthesis in rats (ED₅₀, 32 mg/kg).
YM-53601 free base 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 free base potentiates Doxorubicin-mediated hepatocellular carcinoma cells (HCC) growth arrest and cell death in vivo. "

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