E28362 | PCSK9 inhibitor | Probechem Biochemicals

Chemical Structure : E28362

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E28362 (E 28362)

货号: PC-22461Not For Human Use, Lab Use Only.

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25 mg		Get quote
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	301.35
分子式	C16H19N3O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	6-(2-hydroxypropyl)-4-(p-tolyl)-3,4,6,7-tetrahydro-1H-pyrrolo[3,4-d] pyrimidine-2,5-dione

参考文献

1. Wei-Zhi Wang, et al. Acta Pharmacol Sin. 2024 May 29. doi: 10.1038/s41401-024-01305-9.

E28362 (E 28362)

生物&药学活性

物理化学性质&存储条件

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E28362 (E 28362)

生物&药学活性

物理化学性质&存储条件

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