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FR194738

目录号: PL11748 纯度: ≥98%

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。

CAS No. :204067-52-7

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中文名称	FR194738
英文名称	FR194738
英文别名	FR194738;(E)-N-ethyl-6,6-dimethyl-N-[[3-[2-methyl-2-(thiophen-3-ylmethoxy)propoxy]phenyl]methyl]hept-2-en-4-yn-1-amine;hydrochloride;CID 9869566;(e)-N-ethyl-N-(6,6-dimethyl-2-hepten-4-ynyl)-3-[2-methyl-2-(3-thienyl-methoxy)propyloxy]benzylamine hydrochloride
Cas No.	204067-52-7
分子式	C₂₇H₃₈ClNO₂S
分子量	476.11
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	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。

产品详情	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 IC 50 of 9.8 nM.
性状	Oil
IC50 & Target[1][2]	IC50: 9.8 nM (squalene epoxidase, in HepG2 cell homogenates)
体外研究(In Vitro)	In intact HepG2 cells<, FR194738 concentration-dependently inhibits the incorporation of [C]acetate into free cholesterol and cholesteryl ester, with IC50s of 4.9 and 8.0 nM, respectively. FR194738 induces intracellular [C]squalene accumulation. FR194738 increases the incorporation of [C]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 m
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Sawada M, et al. Effect of FR194738, a potent inhibitor of squalene epoxidase, on cholesterol metabolism in HepG2 cells. Eur J Pharmacol. 2001 Nov 9;431(1):11-6. [2]. Sawada M, et al. Synthesis and biological activity of a novel squalene epoxidase inhibitor, FR194738. Bioorg Med Chem Lett. 2004 Feb 9;14(3):633-7.

溶解度数据	In Vitro: DMSO : 250 mg/mL (525.09 mM; Need ultrasonic)配制储备液

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[1]. Sawada M, et al. Effect of FR194738, a potent inhibitor of squalene epoxidase, on cholesterol metabolism in HepG2 cells. Eur J Pharmacol. 2001 Nov 9;431(1):11-6.
[2]. Sawada M, et al. Synthesis and biological activity of a novel squalene epoxidase inhibitor, FR194738. Bioorg Med Chem Lett. 2004 Feb 9;14(3):633-7.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

FR194738

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