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YM-53601
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
YM-53601图片
CAS NO:182959-33-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
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.
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.
分子量

372.86

性状

Solid

Formula

C21H22ClFN2O

CAS 号

182959-33-7

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6820 mL13.4099 mL26.8197 mL
5 mM0.5364 mL2.6820 mL5.3639 mL
10 mM0.2682 mL1.3410 mL2.6820 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。