| DC74237 |
NYX-PCSK9i
|
NYX-PCSK9i is an orally bioavailable small-molecule inhibitor of PCSK9, inhibits PCSK9-LDLR interaction with IC50 of 323 nM in in vitro biochemical binding assays. |
| DC74236 |
NYX-1492
|
NYX-1492 is a small molecule PCSK9 inhibitor, blocks PCSK9 binding with the LDLR, attenuates inflammation in vascular cells and tissue-engineered blood vessels (TEBVs). |
| DC74235 |
7030B-C5
|
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. |
| DC70533 |
K-312
|
K-312 is a novel cholesteryl ester transfer protein (CETP) inhibitor with IC50 of 60 nM, also suppresses hepatocyte expression of PCSK9, raises HDL and lowers LDL cholesterol levels in vivo; raises HDL cholesterol, decreases LDL cholesterol, and attenuates aortic atherosclerosis in cholesterol-fed rabbits; decreases PCSK9 expression in human primary hepatocytes and in the human hepatoma cell line HepG2, decreases the occupancy of SREBP-1 and SREBP-2 on the sterol regulatory element of the PCSK9 promoter. |
| DC70113 |
13PCSK9i
|
13PCSK9i is a highly potent PCSK9-LDLR disruptor peptide with EC50 of 2 nM, SPR Kd of 6.1 nM and 21 nM for hPCSK9 and mPCSK9.13PCSK9i reduces plasma cholesterol levels and increases hepatic LDLR density in a dose-dependent manner.13PCSK9i functions by a unique, allosteric mechanism and is the smallest molecule identified to date with in vivo PCSK9-LDLR disruptor function. |
