lecimibide

Names

[ Name ]:
lecimibide

[Synonym ]:
N'-(2,4-difluorophenyl)-N-[5-(4,5-diphenyl-1H-imidazol-2-ylthio)pentyl]-N-heptylurea
urea,n'-(2,4-difluorophenyl)-n-[5-[(4,5-diphenyl-1h-imidazol-2-yl)thio]pentyl]-n-heptyl
Lecimibide
Lecimibide (USAN)

Biological Activity

[Description]:

Lecimibide (DuP 128) is a potent and specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor for antihyperlipidemia research[1][2].

[Related Catalog]:

Research Areas >> Metabolic Disease

[In Vitro]

Lecimibide (DuP 128)(10 μM, 24 h)可以抑制 HepG2 细胞 85% 的细胞酯化反应[1]。

[In Vivo]

Lecimibide (DuP 128)(i.v., 2.2 mg/kg/day) 在饲养高脂肪和胆固醇的猪中，显著降低了总血浆甘油三酯和极低密度脂蛋白(VLDL)甘油三酯浓度，分别降低了 36% 和 31%。而对总胆固醇、VLDL 胆固醇、LDL 胆固醇、HDL 胆固醇或 LDL apoB 浓度没有显著影响[2]。

[References]

[1]. L J Wilcox, et al. Secretion of hepatocyte apoB is inhibited by the flavonoids, naringenin and hesperetin, via reduced activity and expression of ACAT2 and MTP. J Lipid Res. 2001 May;42(5):725-34.

[2]. J R Burnett, et al. Inhibition of cholesterol esterification by DuP 128 decreases hepatic apolipoprotein B secretion in vivo: effect of dietary fat and cholesterol. Biochim Biophys Acta. 1998 Jul 31;1393(1):63-79.

Chemical & Physical Properties

[ Density]:
1.21g/cm3

[ Molecular Formula ]:
C₃₄H₄₀F₂N₄OS

[ Molecular Weight ]:
590.76900

[ Exact Mass ]:
590.28900

[ PSA ]:
89.81000

[ LogP ]:
9.80240

[ Index of Refraction ]:
1.613

lecimibide

Names

Biological Activity

Chemical & Physical Properties

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Related Compounds