产品
编 号：F229332
分子式：C21H21FN2O
分子量：336.4
分子式：C21H21FN2O
分子量：336.4
产品类型
规格
价格
是否有货
结构图
CAS No: 182959-28-0
产品详情
生物活性：
YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent. YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.
体内研究：
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.?"Animal Model:Sprague-Dawley (SD) rats weighing 150-170?g
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
Dosage:15 mg/kg
Administration:2 wk of daily treatment by p.o. gavage
Result:Significantly decreased the intratumor cholesterol levels.
体外研究：
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.
YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent. YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.
体内研究：
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.?"Animal Model:Sprague-Dawley (SD) rats weighing 150-170?g
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
Dosage:15 mg/kg
Administration:2 wk of daily treatment by p.o. gavage
Result:Significantly decreased the intratumor cholesterol levels.
体外研究：
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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备