FR194738|cas:204067-52-7|西域试剂

FR194738,98.09%

产品编号：Bellancom-100303A| CAS NO：204067-52-7| 分子式：C₂₇H₃₈ClNO₂S| 分子量：476.11

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-100303A		￥6000.00	杭州北京（现货）
Bellancom-100303A		￥10500.00	杭州北京（现货）

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FR194738

产品介绍

FR194738 是一种角鲨烯环氧化酶 (squalene epoxidase) 抑制剂。在 HepG2 细胞匀浆中, FR194738 抑制角鲨烯环氧酶活性，IC₅₀ 值为 9.8 nM。

生物活性

FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC₅₀ of 9.8 nM.

体外研究

In intact HepG2 cells<, FR194738 concentration-dependently inhibits the incorporation of [¹⁴C]acetate into free cholesterol and cholesteryl ester, with IC₅₀s of 4.9 and 8.0 nM, respectively. FR194738 induces intracellular [¹⁴C]squalene accumulation. FR194738 increases the incorporation of [¹⁴C]acetate into squalene, an intermediate of cholesterol synthesis. FR194738 potently inhibits squalene epoxidase (SE) in HepG2 cell homogenate and liver microsomes in dogs and rats. The inhibitory effect of FR194738 in comparison to the HMG-CoA reductase inhibitors, Simvastatin, Fluvastatin and Pravastatin, on cholesterol biosynthesis in HepG2 cells is examined. Among these compounds, FR194738 is the most potent, with an IC₅₀ of 2.1 nM. The IC₅₀s of Simvastatin, Fluvastatin and Pravastatin are 40, 28 and 5100 nM, respectively. FR194738 inhibits hamster liver microsomal squalene epoxidase activity in a concentration-dependent manner with an IC₅₀ of 14 nM.

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

体内研究

Serum lipid levels in hamsters after daily administration of FR194738 and Pravastatin for 10 d are measured. FR194738 reduces the serum levels of total, non high density lipoprotein (HDL) and HDL cholesterol, and triglyceride. Treatment of hamsters with FR194738 increases HMG-CoA reductase activity by 1.3-fold at 32 mg/kg compared to the control group and does not significantly change that at 100 mg/kg.

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

体内研究

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

性状

Oil

溶解性数据

In Vitro:

DMSO : 250 mg/mL (525.09 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1004 mL	10.5018 mL	21.0035 mL
5 mM	0.4201 mL	2.1004 mL	4.2007 mL
10 mM	0.2100 mL	1.0502 mL	2.1004 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.37 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.37 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.37 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.37 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。