7030B-C5 | PCSK9 inhibitor | Probechem Biochemicals

Chemical Structure : 7030B-C5

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7030B-C5 (PCSK9 inhibitor)

货号: PC-49373Not For Human Use, Lab Use Only.

7030B-C5 is an effective small-molecule PCSK9 inhibitor with IC50 of 1.61 uM (PCSK9 transcription) in HepG2 cells, with no apparent effect on cell growth and survival.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

7030B-C5 is an effective small-molecule PCSK9 inhibitor with IC50 of 1.61 uM (PCSK9 transcription) in HepG2 cells, with no apparent effect on cell growth and survival.
7030B-C5 down-regulated PCSK9 expression and increased the total cellular LDLR protein and its mediated LDL-C uptake by HepG2 cells.
Oral administration of 7030B-C5 (10-30 mg/kg) reduced hepatic and plasma PCSK9 level and increased hepatic LDLR expression in both C57BL/6 J and ApoE KO mice.
7030B-C5 inhibited lesions in en face aortas and aortic root in ApoE KO mice with a slight amelioration of lipid profiles.
Transcriptional regulation of PCSK9 by 7030B-C5 mostly depend on the transcriptional factor HNF1α and FoxO3, FoxO1 was found to play an important role in 7030B-C5 mediated integration of hepatic glucose and lipid metabolism.

物理化学性质&存储条件

分子量	359.386
分子式	C17H21N5O4
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	8-((2-hydroxyethyl)amino)-7-(3-methoxybenzyl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione

参考文献

1. Xuelei Wang, et al. EBioMedicine. 2020 Feb;52:102650.