2. Metabolic Enzyme/Protease
  3. PCSK9
  4. E28362

E28362 is an orally active lipid-lowering agent and a selective PCSK9 antagonist. E28362 blocks the interaction between PCSK9 and LDLR, and induces PCSK9 degradation via the ubiquitin-proteasome pathway. E28362 significantly increases the levels of cell surface and total LDLR proteins, enhances low-density lipoprotein uptake, thereby effectively reducing plasma lipids, hepatic cholesterol and triglyceride levels. E28362 shows no obvious cytotoxicity at high concentrations, and significantly attenuates atherosclerotic lesions in animal models. E28362 is an important molecule in research of hyperlipidemia and atherosclerosis.

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E28362

E28362 Chemical Structure

CAS No. : 930017-01-9

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Based on 1 publication(s) in Google Scholar

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Description

E28362 is an orally active lipid-lowering agent and a selective PCSK9 antagonist. E28362 blocks the interaction between PCSK9 and LDLR, and induces PCSK9 degradation via the ubiquitin-proteasome pathway. E28362 significantly increases the levels of cell surface and total LDLR proteins, enhances low-density lipoprotein uptake, thereby effectively reducing plasma lipids, hepatic cholesterol and triglyceride levels. E28362 shows no obvious cytotoxicity at high concentrations, and significantly attenuates atherosclerotic lesions in animal models. E28362 is an important molecule in research of hyperlipidemia and atherosclerosis[1][2].

In Vitro

E28362 (5-20 μM; 18 h) significantly decreases PCSK9 secretion from HepG2 cells[2].

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

E28362 Related Antibodies

ELISA Assay[2]

Cell Line: HepG2
Concentration: 5, 10, 20 μM
Incubation Time: 18 h
Result: Reduced PCSK9 secretion to ~70 pg/mL at 5 μM, ~80 pg/mL at 10 μM, and ~75 pg/mL at 20 μM, compared to the 0 μM control (~100 pg/mL).
In Vivo

E28362 (administered via oral gavage daily at 6.7-60 mg/kg/day for 4 consecutive weeks) dose-dependently reduces plasma TC, TG and LDL-C levels, decreases hepatic lipid accumulation, and upregulates hepatic LDLR protein levels in golden hamsters, thereby ameliorating hyperlipidemia induced by a high-fat diet[2].
E28362 (administered via oral gavage daily at 20-60 mg/kg/day for 12 consecutive weeks) reduces plasma VLDL-C and LDL-C levels, increases hepatic LDLR protein levels, and significantly decreases atherosclerotic lesion burden in ApoE-/- mice fed a Western diet[2].
E28362 (60 mg/kg/day; oral gavage; daily administration; 12 weeks) reduces plasma TC, TG and LDL-C levels, downregulates plasma and hepatic PCSK9 levels, upregulates hepatic LDLR levels, and significantly decreases atherosclerotic lesion burden in human PCSK9D374Y-overexpressing mice fed a Western-style diet[2].

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

Animal Model: Male golden hamsters (7 weeks old; high-fat diet-induced hyperlipidemia model)[2]
Dosage: 6.7 mg/kg/day; 20 mg/kg/day; 60 mg/kg/day
Administration: i.g.; daily; 4 weeks
Result: Reduced plasma total cholesterol (TC) by 21.50%, triglyceride (TG) by 53.51%, and low-density lipoprotein-cholesterol (LDL-C) by 16.97% at 6.7 mg/kg/day.
Reduced plasma TC by 23.22%, TG by 52.59%, and LDL-C by 43.64% at 20 mg/kg/day.
Reduced plasma TC by 28.97%, TG by 47.10%, and LDL-C by 23.05%, and significantly reduced plasma PCSK9 levels at 60 mg/kg/day.
Significantly reduced liver TC content at all three doses; significantly reduced liver TG content at 20 mg/kg/day.
Reduced hepatic steatosis, ballooning, and lipid droplet accumulation at all doses; significantly reduced plasma alanine aminotransferase (ALT) levels at 60 mg/kg/day.
Significantly increased hepatic LDLR protein levels relative to control at all three doses.
Animal Model: Male C57BL/6J mice (6 weeks old; human PCSK9 D374Y overexpression-induced atherosclerosis model)[2]
Dosage: 60 mg/kg/day
Administration: i.g.; daily; 12 weeks
Result: Significantly reduced plasma TC, TG, and LDL-C levels relative to control.
Confirmed reduced cholesterol levels in VLDL and LDL particle fractions via FPLC analysis.
Significantly reduced en face aortic plaque area and aortic root lesion area relative to control.
Significantly decreased hepatic PCSK9 protein levels and increased hepatic LDLR protein levels relative to control.
Significantly reduced plasma PCSK9 levels.
Molecular Weight

301.34

Formula

C16H19N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC(CN(CC(O)C)C2=O)=C2C(C3=CC=C(C)C=C3)N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 94.51%

SDS (251 KB)

COA (254 KB) LCMS (332 KB)

Handling Instructions (2659 KB)
References
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E28362 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

E28362930017-01-9E 28362E-28362PCSK9Proprotein convertase subtilisin/kexin type 9ApoE-/- miceLDLRLDLubiquitin-proteasome pathwaytriglyceridehyperlipidemiaatherosclerosisHepG2 cellsgolden hamstersInhibitorinhibitorinhibit

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