PCSK9-IN-9

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].

Inclisiran sodium (ALN-PCSsc sodium) is a dual-strand siRNA conjugated with triantennary N-acetylgalactosamine (GalNAc), with antihypertensive activity. It inhibits the transcription of PCSK9, reducing the hepatic synthesis of proprotein convertase subtilisin/kexin type 9, and can be used in cardiovascular disease research.

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 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].

MDK6465, also known as PCSK9-IN-8b, is a novel liver-targeted inhibitor of ribosomal synthesis of proprotein convertase subtilisin/kexin type 9 (PCSK9). MDK6465 has CAS#1900686-46-5. the last 4 digits are used in its name.

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.

PF-06815345 hydrochloride, an orally active potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), has an IC50 value of 13.4 μM. It significantly decreases in vivo PCSK9 levels in mice.

Tafolecimab (IBI-306) is a humanised monoclonal antibody targeting PCSK9, capable of improving multiple lipid parameters (LDL, LDL-C, LDL-CFB, etc.), suitable for studying hypercholesterolaemia and mixed hyperlipidaemia.

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.

Lerodalcibep (LIB003) is a potent, high-affinity inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). It is a recombinant fusion protein comprising a small PCSK9-binding protein fused to human serum albumin (HSA) to significantly extend its circulatory half-life. Lerodalcibep binds to circulating PCSK9 and blocks its interaction with low-density lipoprotein receptors (LDLR) on the hepatocyte surface, preventing lysosomal degradation of the receptors. This mechanism increases the density of LDLR on the liver surface, leading to the highly efficient clearance of LDL-cholesterol (LDL-C) from the blood.

Ongericimab (JS002) is a recombinant humanized monoclonal antibody targeting proprotein convertase subtilisin/kexin type 9 (PCSK9). By blocking the binding of PCSK9 to the low-density lipoprotein receptor (LDLR), the antibody reduces LDLR degradation, thereby increasing hepatic LDL-C uptake and lowering plasma cholesterol levels. It is primarily used to research hypercholesterolemia and cardiovascular risk management.

Ralpancizumab is a highly specialized humanized monoclonal antibody target the human proprotein convertase subtilisin/kexin type 9 with exceptional binding affinity and selectivity, inhibition of the interaction between PCSK9 and the low-density lipoprotein receptor across various preclinical experimental models to enhance the clearance of cholesterol from the systemic circulation during strictly monitored laboratory observation periods.

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].

Anti-PCSK9 Antibody is a humanized monoclonal antibody targeting Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9). PCSK9 is a serine protease primarily secreted by the liver that binds to the Low-Density Lipoprotein Receptor (LDLR) on the hepatocyte surface, promoting its internalization and lysosomal degradation, thereby preventing LDLR recycling to the cell surface. This reduces the liver's ability to clear LDL-cholesterol (LDL-C) from the blood. Anti-PCSK9 Antibody specifically binds to PCSK9, blocking its interaction with LDLR and inhibiting PCSK9-mediated LDLR degradation. This action increases the density of LDLR on hepatocytes, enhances LDL-C clearance, and significantly lowers serum cholesterol levels. It is widely used in research on hypercholesterolemia and atherosclerotic cardiovascular diseases.

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.

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.