E-5324
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.
- CAS No.: 141799-76-0
- Formula: C26H34N4O2
- Molecular Weight:434.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 44 to 190 nM (ACAT)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 141799-76-0
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Molecular Weight 434.57
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Formula C26H34N4O2
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SMILES
O=C(NC1=C(C)C=CC=C1OCCCN2C(CC)=C(C3=CC=CC=C3)N=C2)NCCCC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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