YM-53601|cas:182959-33-7|西域试剂

YM-53601,99.26%

产品编号：Bellancom-100313A| CAS NO：182959-33-7| 分子式：C₂₁H₂₂ClFN₂O| 分子量：372.86

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-100313A		￥3200.00	杭州北京（现货）
Bellancom-100313A		￥13500.00	杭州北京（现货）

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YM-53601

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。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, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC₅₀ of 79 nM. Lipid-lowering agent. YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.

体外研究

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^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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).
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^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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^[4]
Dosage:	15 mg/kg
Administration:	2 wk of daily treatment by p.o. gavage
Result:	Significantly decreased the intratumor cholesterol levels.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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^[4]
Dosage:	15 mg/kg
Administration:	2 wk of daily treatment by p.o. gavage
Result:	Significantly decreased the intratumor cholesterol levels.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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^[4]
Dosage:	15 mg/kg
Administration:	2 wk of daily treatment by p.o. gavage
Result:	Significantly decreased the intratumor cholesterol levels.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (268.20 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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)

参考文献