FR194738 free base
- Product Name
- FR194738 free base
- CAS No.
- 204067-45-8
- Chemical Name
- FR194738 free base
- Synonyms
- FR194738 free base;FR194738 free base, 10 mM in DMSO;FR194738 free base,FR-194738 free base;(E)-N-Ethyl-6,6-dimethyl-N-(3-(2-methyl-2-(thiophen-3-ylmethoxy)propoxy)benzyl)hept-2-en-4-yn-1-amine;Benzenemethanamine, N-[(2E)-6,6-dimethyl-2-hepten-4-yn-1-yl]-N-ethyl-3-[2-methyl-2-(3-thienylmethoxy)propoxy]-
- CBNumber
- CB54797059
- Molecular Formula
- C27H37NO2S
- Formula Weight
- 439.65
- MOL File
- 204067-45-8.mol
FR194738 free base Property
- Boiling point:
- 538.0±50.0 °C(Predicted)
- Density
- 1.051±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Viscous Liquid
- pka
- 7.09±0.50(Predicted)
- color
- Colorless to light yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
FR194738 free base Chemical Properties,Usage,Production
Uses
FR194738 free base is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
Biological Activity
FR194738 free base is a squalene epoxidase inhibitor. In HepG2 cell homogenate, FR194738 inhibits squalene epoxidase activity with IC50 of 9.8 nM.
in vitro
In intact HepG2 cells, FR194738 concentration-dependently inhibits the incorporation of [ 14 C]acetate into free cholesterol and cholesteryl ester, with IC 50 s of 4.9 and 8.0 nM, respectively. FR194738 induces intracellular [ 14 C]squalene accumulation. It increases the incorporation of [ 14 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 IC 50 of 2.1 nM. The IC 50 s 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 IC 50 of 14 nM.
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.
target
IC50: 9.8 nM (squalene epoxidase, in HepG2 cell homogenates)
References
[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. DOI:10.1016/s0014-2999(01)01411-x
[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. DOI:10.1016/j.bmcl.2003.11.072
[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. DOI:10.1248/bpb.25.1577
FR194738 free base Preparation Products And Raw materials
Raw materials
Preparation Products
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