E-5324

Modify Date: 2024-01-02 09:10:54

E-5324 Structure
E-5324 structure
Common Name E-5324
CAS Number 141799-76-0 Molecular Weight 434.57400
Density 1.11g/cm3 Boiling Point 637.4ºC at 760 mmHg
Molecular Formula C26H34N4O2 Melting Point N/A
MSDS N/A Flash Point 339.3ºC

 Use of E-5324


E-5324 is potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with IC50s of 44 to 190 nM.

 Names

Name 1-butyl-3-[2-[3-(5-ethyl-4-phenylimidazol-1-yl)propoxy]-6-methylphenyl]urea
Synonym More Synonyms

 E-5324 Biological Activity

Description E-5324 is potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with IC50s of 44 to 190 nM.
Related Catalog
Target

IC50: 44 to 190 nM (ACAT)[1]

In Vitro E-5324 is a potent ACAT inhibitor with IC50s of 44 to 190 nM in microsomes. E-5324 shows no effect on triglyceride synthesis up to 10 μM. E-5324 also has no effect on bovine pancreatic cholesterol esterase or lecithin: cholesterol acyltransferase (LCAT) up to 10 μM. E-5324 inhibits the incorporation of [3H]oleate into cholesteryl [3H]oleate in a concentration-dependent manner with an IC50 of 0.44 μM. E-5324 also inhibits [3H]cholesteryl ester synthesis with an IC50 of 0.41 μM[1].
In Vivo The areas under the cholesterol-time curves for duration of this study (AUC) for control, E-5324 0.02% and E-5324 0.1% are 104985±4411, 106096±4476 and 105231±4 348 mg×day/dL, respectively. The high dose of E-5324 (0.1%) significantly reduces the surface involvement by 34% and 54% in the aortic arch and thoracic aorta, respectively. E-5324 treatment significantly reduces the wet weight and protein content. In the aortic arch, the high dose of E-5324 (0.1%) significantly reduces both cholesteryl ester and total cholesterol by 60% and 59%, respectively. The high dose of E-5324 (0.1%) markedly reduces the ACAT activities in the aortic arch and thoracic aorta by 35% and 44%, respectively[2].
Cell Assay In the study of the inhibitory effect of E-5324, PMA-treated THP-1 cells are incubated in LPDS/RPMI containing 50 μg protein/mL βVLDL for 5 hr. Then, 100 μL of each concentration of E-5324 solution or vehicle (LPDS/RPMI) is added to the cultured cells. After incubation with E-5324 for 30 min, 20 μL of [3H]oleate-BSA complex is added, and the mixture is incubated for 2 hr. The lipids are extracted from the cells with hexane: 2-propanol (3:2, v/v) and then separated by TLC. The remaining cellular protein is dissolved in 0.1 N NaOH[1].
Animal Admin Forty male WHHL rabbits weighing approximately 1.7 kg at the age of 3 months are used in the experiment. All animals are individually caged and receive 100 g/day of food throughout the experiment. The rabbits are divided into 4 groups so as to make their plasma total cholesterol levels similar. The rabbits are fed a standard rabbit chow, ORC-4, or ORC-4 containing E5324 (0.02% or 0.1% (w/w)), or ORC-4 containing probucol (1% (w/w)) for 16 weeks[2].
References

[1]. Kogushi M, et al. Effect of E5324, a novel inhibitor of acyl-CoA:cholesterol acyltransferase, on cholesteryl ester synthesis and accumulation in macrophages. Jpn J Pharmacol. 1995 Jun;68(2):191-9.

[2]. Kogushi M, et al. Anti-atherosclerotic effect of E5324, an inhibitor of acyl-CoA:cholesterol acyltransferase, in Watanabe heritable hyperlipidemic rabbits. Atherosclerosis. 1996 Aug 2;124(2):203-10.

 Chemical & Physical Properties

Density 1.11g/cm3
Boiling Point 637.4ºC at 760 mmHg
Molecular Formula C26H34N4O2
Molecular Weight 434.57400
Flash Point 339.3ºC
Exact Mass 434.26800
PSA 71.67000
LogP 6.08900
Vapour Pressure 3.78E-16mmHg at 25°C
Index of Refraction 1.576
Storage condition 2-8℃

 Synthetic Route

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E-5324 Structure

E-5324

CAS#:141799-76-0

Literature: Kimura; Watanabe; Matsui; Hayashi; Tanaka; Ohtsuka; Saeki; Kogushi; Kabayashi; Akasaka; Yamagishi; Saitou; Yamatsu Journal of Medicinal Chemistry, 1993 , vol. 36, # 11 p. 1641 - 1653

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E-5324 Structure

E-5324

CAS#:141799-76-0

Literature: Kimura; Watanabe; Matsui; Hayashi; Tanaka; Ohtsuka; Saeki; Kogushi; Kabayashi; Akasaka; Yamagishi; Saitou; Yamatsu Journal of Medicinal Chemistry, 1993 , vol. 36, # 11 p. 1641 - 1653

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E-5324 Structure

E-5324

CAS#:141799-76-0

Literature: Kimura; Watanabe; Matsui; Hayashi; Tanaka; Ohtsuka; Saeki; Kogushi; Kabayashi; Akasaka; Yamagishi; Saitou; Yamatsu Journal of Medicinal Chemistry, 1993 , vol. 36, # 11 p. 1641 - 1653

~%

E-5324 Structure

E-5324

CAS#:141799-76-0

Literature: Kimura; Watanabe; Matsui; Hayashi; Tanaka; Ohtsuka; Saeki; Kogushi; Kabayashi; Akasaka; Yamagishi; Saitou; Yamatsu Journal of Medicinal Chemistry, 1993 , vol. 36, # 11 p. 1641 - 1653

~%

E-5324 Structure

E-5324

CAS#:141799-76-0

Literature: Kimura; Watanabe; Matsui; Hayashi; Tanaka; Ohtsuka; Saeki; Kogushi; Kabayashi; Akasaka; Yamagishi; Saitou; Yamatsu Journal of Medicinal Chemistry, 1993 , vol. 36, # 11 p. 1641 - 1653

~%

E-5324 Structure

E-5324

CAS#:141799-76-0

Literature: Kimura; Watanabe; Matsui; Hayashi; Tanaka; Ohtsuka; Saeki; Kogushi; Kabayashi; Akasaka; Yamagishi; Saitou; Yamatsu Journal of Medicinal Chemistry, 1993 , vol. 36, # 11 p. 1641 - 1653

~98%

E-5324 Structure

E-5324

CAS#:141799-76-0

Literature: Kimura; Watanabe; Matsui; Hayashi; Tanaka; Ohtsuka; Saeki; Kogushi; Kabayashi; Akasaka; Yamagishi; Saitou; Yamatsu Journal of Medicinal Chemistry, 1993 , vol. 36, # 11 p. 1641 - 1653

 Synonyms

e-5324
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