FR-194738
- CAS No.
- 204067-52-7
- Chemical Name:
- FR-194738
- Synonyms
- FR-194738;FR194738,FR-194738;FR194738 hydrochloride;(E)-N-ethyl-6,6-dimethyl-N-[[3-[2-methyl-2-(thiophen-3-ylmethoxy)propoxy]phenyl]methyl]hept-2-en-4-yn-1-amine;(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
- CBNumber:
- CB62627889
- Molecular Formula:
- C27H38ClNO2S
- Molecular Weight:
- 476.12
- MDL Number:
- MFCD22572763
- MOL File:
- 204067-52-7.mol
FR-194738 Chemical Properties,Uses,Production
Biological Activity
FR194738 is a squalene epoxidase inhibitor. In HepG2 cell homogenate, It inhibits squalene epoxidase activity with IC50 of 9.8 nM.
in vitro
In intact HepG2 cells14C]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 sub> 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.
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in vivo
Serum lipid levels in hamsters after daily administration of FR194738 and Pravastatin for 10 d are measured. It 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)
FR-194738 Preparation Products And Raw materials
Raw materials
Preparation Products
FR-194738 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49739 | 58 |
DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
Absin Bioscience Inc. | 021-38015121 15000105423 | chenjw@absin.cn | China | 24734 | 58 |
cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 9946 | 58 |
Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 | psaitong@jm-bio.com | China | 29778 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24131 | 58 |
Nanjing Shizhou Biology Technology Co.,Ltd | 025-85560043 15850508050 | cindy.huang@synzest.com | China | 12007 | 58 |