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FR194738 free base

Catalog No. T11321 CAS 204067-45-8

FR194738 free base inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.

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FR194738 free base, CAS 204067-45-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 233.00
5 mg	In stock	$ 497.00
10 mg	In stock	$ 723.00
25 mg	In stock	$ 1,130.00
50 mg	In stock	$ 1,520.00
100 mg	In stock	$ 1,980.00
1 mL * 10 mM (in DMSO)	In stock	$ 547.00

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Purity: 99.65%

Biological Description

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Description	FR194738 free base inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
Targets&IC50	SE (HepG2 cell homogenates):9.8 nM
In vitro	FR194738 free base potently inhibits squalene epoxidase in HepG2 cell homogenate and liver microsomes in dogs and rats. FR194738 free base inhibits hamster liver microsomal squalene epoxidase activity in a concentration-dependent manner with an IC50 of 14 nM[2]. In intact HepG2 cells, FR194738 free base inhibits the incorporation of [14C]acetate into free cholesterol and cholesteryl ester in a concentration-dependent manner(IC50s = 4.9 and 8.0 nM). FR194738 free base induces intracellular [14C]squalene accumulation and increases the incorporation of [14C]acetate into squalene[3].
In vivo	FR194738 free base reduces the serum levels of total, non high density lipoprotein and high density lipoprotein cholesterol, and triglyceride. In hamsters, FR194738 free base(32 mg/kg) increases HMG-CoA reductase activity by 1.3-fold[2].

Molecular Weight	439.65
Formula	C27H37NO2S
CAS No.	204067-45-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/mL (204.7 mM), Sonification is recommended.

References and Literature

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. 3. Sawada M, et al. Inhibition of cholesterol synthesis causes both hypercholesterolemia and hypocholesterolemia in hamsters. Biol Pharm Bull. 2002 Dec;25(12):1577-82.

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Keywords

FR194738 free base 204067-45-8 Microbiology/Virology Antifungal FR 194738 FR194738 FR-194738 free base FR-194738 inhibitor inhibit

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