pcsk9

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.

AZD0780 (EX-A6975) is an oral small molecule PCSK9 inhibitor being developed by AstraZeneca as a first-in-class treatment for patients with dyslipidemia that is uncontrolled with statins alone.

Alirocumab is a human monoclonal antibody that inhibits PCSK9. It is produced by recombinant DNA technology in Chinese hamster ovary cell suspension culture.

Evolocumab is an inhibitor of the humanized monoclonal antibody PCSK9. It binds to circulating PCSK9 protein, resulting in inhibition of PCSK9 binding to LDLR. It can be used in studies of hypercholesterolemia and atherosclerotic cardiovascular disease.

PF-06446846 hydrochloride, an orally active and highly selective inhibitor, targets Proprotein Convertase Subtilisin Kexin type 9 (PCSK9) translation by inducing ribosomal stalling at approximately codon 34, effectively suppressing PCSK9 expression.

R-IMPP is an inhibitor of PCSK9 translation. R-IMPP stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin.

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.

Bococizumab(PF-04950615) is a humanized mAb against PCSK9 and an inhibitor of the synthesis of PCSK9 in the liver that reduces the amount of low-density lipoprotein cholesterol (LDL-C) in the blood.Bococizumab is used to treat hypercholesterolemia.

Frovocimab (LY 3015014) is a humanized IgG4 monoclonal antibody to Subtilisin/Kexin Protein Converting Enzyme Type 9 (PCSK9) that binds to the catalytic domain of PCSK9 and lowers low-density lipoprotein cholesterol (LDL-C) in patients with hypercholesterolemia.Frovocimab is used in the study of hypercholesterolemia. Frovocimab is used to study hypercholesterolemia.

Lodelcizumab (LGT 209) is a monoclonal antibody targeting the preprotein convertase Bacillus subtilis protease Kexin-9 (PCSK9) and is used to study hypercholesterolemia.

RG-7652 is a humanized monoclonal antibody targeting PCSK9 for the study of cardiovascular disease.

Pinostrobin, a potent flavonoid inducer, exerts a neuroprotective effect against Aα²(25-35)-induced neurotoxicity in PC12 cells, at least in part, via inhibiting oxidative damage and calcium overload, as well as suppressing the mitochondrial pathway of ce

Pep 2-8 ammonium salt is Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. Potent inhibitor of PCSK9 binding to LDL receptor (IC50 = 0.8 μM). Restores LDL uptake in HepG2 cells treated with PCSK9.

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-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-IN-30 (Compound 3f), a PCSK9 inhibitor, effectively targets a cryptic binding groove on PCSK9, thereby preventing PCSK9 from associating with the low-density lipoprotein receptor (LDLR) (IC 50 = 537 nM). This inhibition aids in the restoration of low-density lipoprotein (LDL) uptake by liver cells and significantly reduces plasma cholesterol levels. Demonstrating good bioavailability in mice, PCSK9-IN-30 holds potential for research within cardiovascular disease contexts.

PCSK9-IN-32 (compound 8) acts as an inhibitor of PCSK9[1:33]-GFP translation.

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-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 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].