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Chemical Structure : 7030B-C5
Catalog No.: 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.
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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.
| M.Wt | 359.386 | |
| Formula | C17H21N5O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Xuelei Wang, et al. EBioMedicine. 2020 Feb;52:102650.
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