YM-53601 - CAS:182959-33-7

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YM-53601

目录号 : KCM12127 CAS No. : 182959-33-7 纯度 : ≥98%

Data Sheet SDS 产品使用指南

YM-53601 is a squalene synthase inhibitor (ICs = 79 and 90 nM in HepG2 cells and rat liver microsomes, respectively). It inhibits cholesterol biosynthesis in rats (ED = 32 mg/kg). YM-53601 dose-dependently reduces plasma triglyceride and non-HDL cholesterol levels in hamsters fed both normal and high-fat diets. It also reduces viral RNA, core and NS3 protein production, and secreted viral particles in Huh7.5.1-8 cells infected with the hepatitis C virus (HCV) strain JFH-1 without affecting cell viability at concentrations ranging from 0.5 to 1.5 μM. YM-53601 (1-10 μM) confers protection against cytotoxicity induced by the bacterial pore-forming toxin pneumolysin in HBE1 and normal human bronchial epithelial (NHBE) cells.

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
1mg		In-stock
5mg		In-stock

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YM-53601 In-stock

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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 activity in hepatic microsomes of several rat, hamster, guinea pig, rhesus monkey, and human HepG2 cell lines, with IC₅₀ values of 90, 170, 46, 45, and 79 nM, respectively.
YM-53601 inhibits the conversion of [3H]farnesyl diphosphate to [3H]squalene by hamster hepatic squalene synthase, with an IC₅₀ of 170 nM.
YM-53601 (1 μM) enhances the sensitivity of H35 cells to toxic carotene, lonidamine, and doxorubicin. YM-53601 (1 μM) reduces mitochondrial cholesterol levels in H35 and HepG2 cells.

Cell Viability Assay

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

YM-53601 inhibits cholesterol biosynthesis in rats (ED50, 32 mg/kg).
YM-53601 also reduces plasma non high density lipoprotein cholesterol levels in hamsters at an oral dose of 50 mg/kg/day for 5 days, approximately 70%.
YM-53601 enhances doxorubicin mediated growth arrest and in vivo cell death in hepatocellular carcinoma (HCC) cells.

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.

分子式

C₂₁H₂₁FN₂O^.HCl

分子量

372.86

CAS号

182959-33-7

中文名称

9H-咔唑，2-[（2E）-2-（1-氮杂双环[2.2.2]辛-3-亚基）-2-氟乙氧基]-，一盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°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°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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.70 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.70 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.70 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度： ≥98%

Data Sheet

SDS

产品使用指南

Joan Montero,et al.Mitochondrial cholesterol contributes to chemotherapy resistance in hepatocellular carcinoma. Cancer Res. 2008 Jul 1;68(13):5246-56.

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器