Chemical Structure : E28362
CAS No.:
930017-01-9
E28362
(E 28362)
Catalog No.: PC-22461Not For Human Use, Lab Use Only.
E28362 is a novel small-molecule PCSK9 inhibitor, effectively binds to PCSK9 (SPR KD=14.8 uM) and disrupts the PCSK9-LDLR interaction, promotes the degradation of PCSK9 via the ubiquitin-proteasome pathway.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
E28362 is a novel small-molecule PCSK9 inhibitor, effectively binds to PCSK9 (SPR KD=14.8 uM) and disrupts the PCSK9-LDLR interaction, promotes the degradation of PCSK9 via the ubiquitin-proteasome pathway.
E28362 (5, 10, 20 μM) could significantly increase the intake of DiI-LDL in AML12 cells, with no obvious toxicity.
E28362 increases the LDLR protein level in HepG2 and AML12 cells.
E28362 (6.7, 20, or 60 mg/kg per day) for 4 weeks improves dyslipidemia and decreases hepatic lipid accumulation in HFD-induced golden hamsters.
E28362 (30 or 60 mg/kg per day) for 12 weeks inhibits the development of atherosclerosis in ApoE−/− mice.
E28362 induces PCSK9 degradation through the ubiquitin-proteasome pathway after binding to PCSK9 in hepatic cells.
E28362 decreased PCSK9 levels and alleviated the development of atherosclerosis in PCSK9 overexpression mice.
Physicochemical Properties
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M.Wt
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301.35
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Formula
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C16H19N3O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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6-(2-hydroxypropyl)-4-(p-tolyl)-3,4,6,7-tetrahydro-1H-pyrrolo[3,4-d] pyrimidine-2,5-dione
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References
1. Wei-Zhi Wang, et al. Acta Pharmacol Sin. 2024 May 29. doi: 10.1038/s41401-024-01305-9.
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