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[2]。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。
| 生物活性 | YM-53601, asqualene synthaseinhibitor, reduces plasmacholesteroland triglyceride levels in vivo[1]. YM-53601 inhibits squalene synthase derived from human hepatoma cells with anIC50of 79 nM. Lipid-lowering agent[2]. YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogatesHCVpropagation[3]. |
体外研究
(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[1].
YM-53601 inhibits conversion of [3H]farnesyl diphosphate to [3H]squalene by hamster liver squalene synthase with the IC50 of 170 nM[2].
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[4].
Cell Viability Assay[4] | Cell Line: | H35 and HepG2 cells | | Concentration: | 1 μM | | Incubation Time: | 24 hours | | Result: | Reduced the mitochondrial cholesterol levels in both H35 and HepG2 cells. |
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体内研究
(In Vivo) | YM-53601 suppresses cholesterol biosynthesis in rats (ED50, 32 mg/kg)[1].
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[2].
YM-53601 potentiates Doxorubicin-mediated hepatocellular carcinoma cells (HCC) growth arrest and cell death in vivo[4].
| Animal Model: | Sprague-Dawley (SD) rats weighing 150-170 g[1] | | Dosage: | 6.25, 12.5, 25 or 50 mg/kg | | Administration: | Given a single p.o. | | Result: | Inhibited cholesterol biosynthesis from acetate in a dose-dependent manner in rats. The ED50 value for YM-53601 cholesterol biosynthesis inhibition is 32 mg/kg. |
| Animal Model: | Five- to six-week-old male BALB/c athymic (nu/nu) nude mice[4] | | Dosage: | 15 mg/kg | | Administration: | 2 wk of daily treatment by p.o. gavage | | Result: | Significantly decreased the intratumor cholesterol levels. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(268.20 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.6820 mL | 13.4099 mL | 26.8197 mL | | 5 mM | 0.5364 mL | 2.6820 mL | 5.3639 mL | | 10 mM | 0.2682 mL | 1.3410 mL | 2.6820 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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