E28362
Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 94.51%
- CAS 番号: 930017-01-9
- 分子式: C16H19N3O3
- 分子量:301.34
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
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Cell Line:HepG2
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Concentration:5, 10, 20 μM
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Incubation Time:18 h
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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).
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.
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Animal Model:Male golden hamsters (7 weeks old; high-fat diet-induced hyperlipidemia model)[2]
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Dosage:6.7 mg/kg/day; 20 mg/kg/day; 60 mg/kg/day
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Administration:i.g.; daily; 4 weeks
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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.
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Animal Model:Male C57BL/6J mice (6 weeks old; human PCSK9 D374Y overexpression-induced atherosclerosis model)[2]
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Dosage:60 mg/kg/day
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Administration:i.g.; daily; 12 weeks
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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.
化学情報
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CAS 番号 930017-01-9
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性状 Solid
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分子量 301.34
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分子式 C16H19N3O3
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Color White to off-white
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SMILES
O=C1NC(CN(CC(O)C)C2=O)=C2C(C3=CC=C(C)C=C3)N1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Yue J, et al. Chemotherapy-Induced Bone Marrow Suppression: A Bibliometrics Analysis. J Multidiscip Healthc. 2025;18:1895-1911. Published 2025 Apr 7. [Content Brief]
[2]. Wang WZ, et al. A novel small-molecule PCSK9 inhibitor E28362 ameliorates hyperlipidemia and atherosclerosis. Acta Pharmacol Sin. 2024;45(10):2119-2133. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
E28362 関連分類
HY-162562 関連分類
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