1. Metabolic Enzyme/Protease Anti-infection
  2. Farnesyl Transferase HCV
  3. YM-53601

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。

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YM-53601 Chemical Structure

YM-53601 Chemical Structure

CAS No. : 182959-33-7

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规格 价格 是否有货 数量
1 mg ¥3200
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Other Forms of YM-53601:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo[1]. YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent[2]. YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation[3].

体外研究
(In Vitro)

YM-53601 抑制几种大鼠、仓鼠、豚鼠、恒河猴和人源 HepG2 细胞的肝微粒体中的角鲨烯合酶活性,IC50 为 90、170、46、45,和 79 nM[1]
YM-53601 抑制仓鼠肝脏角鲨烯合酶将[3H]法尼基二磷酸转化为[3H]角鲨烯IC50 为 170 nM[2]
YM-53601 (1 μM) 增强 H35 细胞对毒胡萝卜素、lonidamine 和阿霉素的敏感性。YM-53601 (1 μM) 降低 H35 和 HepG2 细胞中的线粒体胆固醇水平[4]

MCE 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 抑制大鼠胆固醇生物合成 (ED50,32 mg/kg)[1]
YM-53601 还降低血浆非高密度脂蛋白胆固醇水平在仓鼠中,口服剂量为 50 mg/kg/天,持续 5 天,约 70%[2]
YM-53601 增强多柔比星介导的肝细胞癌细胞 (HCC) 生长停滞和体内细胞死亡[4]

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

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

Formula

C21H22ClFN2O

CAS 号
性状

固体

颜色

Off-white to light brown

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 中的溶解度 : 100 mg/mL (268.20 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.26%

参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6820 mL 13.4099 mL 26.8197 mL 67.0493 mL
5 mM 0.5364 mL 2.6820 mL 5.3639 mL 13.4099 mL
10 mM 0.2682 mL 1.3410 mL 2.6820 mL 6.7049 mL
15 mM 0.1788 mL 0.8940 mL 1.7880 mL 4.4700 mL
20 mM 0.1341 mL 0.6705 mL 1.3410 mL 3.3525 mL
25 mM 0.1073 mL 0.5364 mL 1.0728 mL 2.6820 mL
30 mM 0.0894 mL 0.4470 mL 0.8940 mL 2.2350 mL
40 mM 0.0670 mL 0.3352 mL 0.6705 mL 1.6762 mL
50 mM 0.0536 mL 0.2682 mL 0.5364 mL 1.3410 mL
60 mM 0.0447 mL 0.2235 mL 0.4470 mL 1.1175 mL
80 mM 0.0335 mL 0.1676 mL 0.3352 mL 0.8381 mL
100 mM 0.0268 mL 0.1341 mL 0.2682 mL 0.6705 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
YM-53601
目录号:
HY-100313A
需求量: