1. Metabolic Enzyme/Protease
  2. Acyltransferase

E-5324 

Cat. No.: HY-19183
Handling Instructions

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

For research use only. We do not sell to patients.

E-5324 Chemical Structure

E-5324 Chemical Structure

CAS No. : 141799-76-0

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & 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].

References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

434.57

Formula

C₂₆H₃₄N₄O₂

CAS No.

141799-76-0

SMILES

O=C(NC1=C(C)C=CC=C1OCCCN2C(CC)=C(C3=CC=CC=C3)N=C2)NCCCC

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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E-5324
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HY-19183
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E-5324

Cat. No.: HY-19183