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-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 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 is a potent inhibitor of PCSK9, effectively preventing the binding of PCSK9 to low-density lipoprotein (LDL) receptors through its mechanism of action. It exhibits this inhibitory activity with an IC 50 value of 537 nM.

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-23 (compound 5C), a potent inhibitor of PCSK9, effectively blocks the secretion of PCSK9 from HepG2 cells and significantly enhances the expression of the LDL receptor (LDLR) [1].

Anti-PCSK9 Antibody is a CHO-expressed human antibody targeting PCSK9. It features a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. For isotype control, refer to HumanIgG1kappa, Isotype Control.

PCSK9-IN-28 (Compound C11) is a PCSK9 inhibitor that can be isolated from Euphorbia esula. It functions by binding to HNF1α, affecting its nuclear distribution, and thereby inhibiting PCSK9 transcription, which in turn enhances LDLR and promotes LDL uptake. In a high-fat diet (HFD) mouse model, PCSK9-IN-28 demonstrates significant lipid-lowering activity and can be utilized for hyperlipidemia research.