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Cat. No.: HY-19183

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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

Storage:

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

Data Sheet (277 KB)

E-5324 Chemical Structure

CAS No.: 141799-76-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

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]

All Acyltransferase Isoforms :

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].

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

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].

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

Chemical Information

CAS No. 141799-76-0
Molecular Weight 434.57
Formula C₂₆H₃₄N₄O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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