pcsk 9

PCSK9-IN-11 (compound 5r) is a potent PCSK9 inhibitor with oral activity, exhibiting inhibitory activity on PCSK9 transcription in HepG2 cells (IC50 = 5.7 μM) and capable of increasing LDL receptor (LDLR) protein levels. PCSK9-IN-11 is applicable for atherosclerosis research.

PCSK9 ligand 1 is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9(Ki of 107 nM).

PCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 µM. By enhancing the expression of Low-Density Lipoprotein Receptor (LDLR) protein and reducing PCSK9 expression, PCSK9-IN-10 effectively decreases atherosclerosis progression. This compound holds promise for hyperlipidemia research applications.

PCSK9-IN-2 is a newly developed small molecule that effectively inhibits the protein-protein interaction (PPI) between PCSK9 and LDLR. It has been found to have a potent inhibitory activity with an IC50 value of 7.57 μM.

PCSK9 degrader 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) degrader. PCSK9 degrader 1 does not affect PCSK9 function.

PCSK9-IN-29 serves as a lipid-lowering agent that enhances the expression of low-density lipoprotein receptor (LDLR) protein and reduces PCSK9 protein expression in hepG2 cells. Additionally, in crab-eating macaques on a high-fat diet, it lowers serum LDL-C, TC, and liver enzyme ALT levels, reduces body weight and fat, and boosts bone mineral content. PCSK9-IN-29 is useful for studies involving non-alcoholic fatty liver disease and obesity.

PCSK9 autophagic degrader 2 (W6) is an autophagosome-targeting agent for PCSK9, with a DC50 value of 20.6 nM. It exhibits effects comparable to anti-atherosclerotic treatments and has a binding constant (KD) with LC3B of 2.5 μM.

PCSK9ligand 2 is the target protein ligand of PROTACPCSK9 autophagic degrader 2, and it is applicable for research related to anti-atherosclerosis.

PCSK9-IN-27 (Compound 108) is a PCSK9 inhibitor with an IC50 value of 3.4 nM. It reduces the degradation of LDLR and enhances the uptake of LDL-C.

PCSK9-IN-33 (Compound 1'f) is a PCSK9 inhibitor with an IC50 of 161 nM, which can be utilized in hypercholesterolemia research.

PCSK9 modulator-2 (Compound 1) is a potent PCSK9 modulator (EC 50 = 202 nM) with potential applications in hyperlipidemia research. Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a recently validated therapeutic target for lowering low-density lipoprotein cholesterol (LDL-C) [1].

PCSK9 modulator-3 (Compound 13) is a potent PCSK9 modulator with an EC50 value of 2.46 nM, showing potential in hyperlipidemia research. PCSK9 is a newly established target for lowering low-density lipoprotein cholesterol (LDL-C) [1].

PCSK9 modulator-4 (Compound 21) is a potent PCSK9 modulator (EC50 = 0.15 nM) utilized in hyperlipidemia research, targeting the recently validated low-density lipoprotein cholesterol (LDL-C) lowering mechanism [1].

PCSK9-IN-13 (compound 3f) is a potent PCSK9 inhibitor with an IC50 of 537 nM. It antagonizes the binding of the low-density lipoprotein receptor (LDLR) to PCSK9 by interacting with a cryptic binding groove on the PCSK9 protein. Since PCSK9 normally mediates the degradation of LDLR, this inhibitor helps maintain higher levels of LDLR on the hepatocyte surface, thereby promoting the uptake of circulating LDL-C. It is a valuable tool for researching novel cholesterol-lowering therapies and cardiovascular disease prevention.

PCSK9-IN-3 is a next-generation tricyclic peptide inhibitor of PCSK9, characterized by its novel structure, high potency, and oral bioavailability.

PCSK9-IN-18 (compound 188) is a potent PCSK9 inhibitor with a K_D value of <200 nM [1].

PCSK9-IN-9, a natural isocoumarin, inhibits proprotein convertase subtilisin-kexin type 9 (PCSK9), IDOL, and SREBP2 mRNA expression, demonstrating specificity by inhibiting PCSK9 with an IC50 value of 11.9 μM [1].

PCSK9-IN-14, also known as compound Ia-8, is a potent inhibitor of PCSK9 [1].

PCSK9-IN-15 (compound 5) is a potent inhibitor of proprotein convertase subtilisin/kexin 9 (PCSK9, K D <200 nM) that plays a crucial role in cholesterol metabolism by regulating blood levels of low-density lipoprotein cholesterol (LDL-C). This compound is useful for researching cholesterol-lowering therapies and dyslipidemia [1].

PCSK9-IN-16, holds potential for research into hypercholesterolemia and other cardiovascular diseases [1].

PCSK9-IN-17 is a PCSK9 inhibitor employed in cholesterol metabolism research.

PCSK9-IN-19 (Compound 1), a PCSK9 inhibitor, is utilized in researching the treatment of high LDL-cholesterol levels and the prevention of coronary artery disease [1].

PCSK9-IN-20 (Compound 3i) is a PCSK9 inhibitor with an IC50 value of 3.96 µM, which reduces PCSK9 and enhances LDLR protein levels in vitro [1].

PCSK9-IN-22 (compound 29), an orally active PCSK9 inhibitor, prevents the protein from interacting with LDLR in vivo [1].