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PCSK9

Brief Information

Name:Proprotein convertase subtilisin kexin type 9
Target Synonym:FHCL3,EC 3.4.21,EC 3.4.21.111,Neural apoptosis-regulated convertase 1,Proprotein convertase 9,NARC1,PSEC0052,PCSK9,NARC-1,EC:3.4.21.-,Proprotein Convertase Subtilisin/Kexin Type 9,Subtilisin/Kexin-Like Protease PC9,PC9,Convertase Subtilisin/Kexin Type 9 P
Number of Launched Drugs:2
Number of Drugs in Clinical Trials:16
Lastest Research Phase:Approved

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Part of Bioactivity data

PCY-H5225-Cell-based assay
FACS assay shows that recombinant Biotinylated FACS

FACS analysis shows that Human PCSK9 (D374Y), His Tag (Cat. No. PCY-H5225) inhibits LDL uptake in HepG2 cells. The EC50 for this effect is 0.0689-0.3049 μg/mL.

PCY-H5225-Cell-based assay
FACS assay shows that recombinant Biotinylated FACS

FACS analysis shows that the effect of Human PCSK9 (D374Y), His Tag (Cat. No. PCY-H5225) inhibiting LDL uptake in HepG2 cells was neutralized by Anti-Human PCSK9 antibody. The concentration of PCSK9 used is 5 μg/mL. The EC50 for Anti-Human PCSK9 antibody is 6.816-12.67 μg/mL.

PC9-H5256-BLI
Human_FcRn_Heterodimer_Protein_Bli

Loaded Human PCSK9, Fc Tag (Cat. No. PC9-H5256) on Protein A Biosensor, can bind Human LDL R, His Tag (Cat. No. LDR-H5224) with an affinity constant of 12.7 nM as determined in BLI assay (ForteBio Octet Red96e) (Routinely tested).

PC9-H52E4-BLI
Human_FcRn_Heterodimer_Protein_Bli

Loaded Human LDL R, Fc Tag (Cat. No. LDR-H5254) on Protein A Biosensor, can bind Hamster PCSK9, His Tag (Cat. No. PC9-H52E4) with an affinity constant of 4.09 nM as determined in BLI assay (ForteBio Octet Red96e) (Routinely tested).

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Synonym Name

PCSK9,FH3,HCHOLA3,LDLCQ1,NARC1,PC9

Background

Proprotein convertase subtilisin/kexin type 9 (PCSK9), is an enzyme which in humans is encoded by the PCSK9 gene.This gene encodes a proprotein convertase belonging to the proteinase K subfamily of the secretory subtilase family. This protein plays a major regulatory role in cholesterol homeostasis. PCSK9 binds to the epidermal growth factor-like repeat A (EGF-A) domain of the low-density lipoprotein receptor (LDLR), inducing LDLR degradation. PCSK9 may also have a role in the differentiation of cortical neurons. Mutations in this gene have been associated with a rare form of autosomal dominant familial hypercholesterolemia (HCHOLA3).

Clinical and Translational Updates

Related Molecule

Public Drug Information

Name Research Code Research Phase Company First Brand Name First Approved Country First Indication First Approved Company First Approved Date Indications Clinical Trials
Alirocumab 316P; REGN-727; SAR-236553 Approved Sanofi, Regeneron Pharmaceuticals Inc 波立达, Praluent Mainland China Dyslipidemias; Hypercholesterolemia; Atherosclerosis s:21:"Sanofi-Aventis Groupe"; 2015-07-24 Homozygous familial hypercholesterolemia; Atherosclerosis; Hypercholesterolemia; Acute Coronary Syndrome; Heterozygous familial hypercholesterolemia; Dyslipidemias; Hyperlipoproteinemia Type II Details
Evolocumab AMG-145 Approved Amgen Inc, Astellas Pharma Inc 瑞百安, Repatha Mainland China Atherosclerosis; Homozygous familial hypercholesterolemia s:9:"Amgen Inc"; 2015-07-17 Homozygous familial hypercholesterolemia; Myocardial Infarction; Diabetes Mellitus, Type 2; Atherosclerosis; Hypercholesterolemia; Coronary Artery Disease; Stroke; Coronary Disease; Heterozygous familial hypercholesterolemia; Dyslipidemias; Cardiovascular Diseases; Diabetes Mellitus; Hyperlipoproteinemia Type II; Hyperlipidemias Details
Inclisiran sodium ALN-60212; PCSK9si; ALN-PCSsc; KJX839; KJX-839 Approved Alnylam Pharmaceuticals Inc Leqvio EU Dyslipidemias; Hypercholesterolemia s:22:"Novartis Europharm Ltd"; 2020-12-09 Plaque, Atherosclerotic; Homozygous familial hypercholesterolemia; Atherosclerosis; Diabetes Mellitus, Type 2; Hypercholesterolemia; Kidney Diseases; Hypolipoproteinemias; Acute Coronary Syndrome; Heterozygous familial hypercholesterolemia; Dyslipidemias; Diabetes Mellitus; Hyperlipoproteinemia Type II; Hyperlipidemias Details

Clinical Drug Information

Name Research Code Research Phase Company Indications Clinical Trials
Frovocimab LY-3015014 Phase 2 Clinical Eli Lilly And Company Hypercholesterolemia; Hyperlipidemias Details
CiVi-007 CiVi-007; LNA-PCSK -9; LNA-PCSK9-GalNac Phase 2 Clinical F. Hoffmann-La Roche Ltd Hypercholesterolemia Details
PCSK9 modulator (Genekey Biotech) Phase 1 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Metabolic Diseases; Inflammation Details
Anti-PCSK9 monoclonal antibody (Biocad) Phase 1 Clinical Biocad Cardiovascular Diseases Details
ATH-04 ATH-04 Phase 1 Clinical Affiris Atherosclerosis Details
SAL-092 SAL092; SAL-092 Phase 1 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Hypercholesterolemia; Dyslipidemias Details
Recombinant human anti-PCSK9 monoclonal antibody (Tasly Pharm) B1655; B-1655 Phase 1 Clinical Tianjin Tasly Pharmaceutical Co Ltd Hypercholesterolemia Details
Recombinant human anti-PCSK9 monoclonal antibody (Salubris) SAL003 Phase 1 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Hypercholesterolemia; Dyslipidemias Details
DC-371739 DC-371739 Phase 1 Clinical Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Hypercholesterolemia; Dyslipidemias; Hyperlipidemias Details
JS-002 JS-002 Phase 3 Clinical Shanghai Junshi Biosciences Co Ltd Hypertriglyceridemia; Atherosclerosis; Hypercholesterolemia; Hyperlipidemia, Familial Combined; Hyperlipidemias Details
CVI-LM001 C-8304; CVI-LM001 Phase 2 Clinical Xiwei'Ai Medicine Technology (Shanghai) Co Ltd Hypercholesterolemia; Hyperlipidemias Details
Lerodalcibep LIB-003 Phase 3 Clinical Lib Therapeutics Hypercholesterolemia; Stroke; Heterozygous familial hypercholesterolemia; Hyperlipoproteinemia Type II Details
AK-102 AK-102 Phase 2 Clinical Zhongshan Akeso Biopharma Co Ltd, Yabao Us Pharmaceutical Co Ltd Homozygous familial hypercholesterolemia; Hypercholesterolemia; Heterozygous familial hypercholesterolemia; Hyperlipidemias; Hyperlipoproteinemia Type II Details
Tafolecimab IBI-306 Phase 3 Clinical Innovent Biologics(Suzhou) Co Ltd Homozygous familial hypercholesterolemia; Hypercholesterolemia; Heterozygous familial hypercholesterolemia Details
SHR-1209 SHR-1209 Phase 3 Clinical Jiangsu Hengrui Medicine Co Ltd Hypercholesterolemia; Hyperlipoproteinemia Type V; Hyperlipidemias; Hyperlipoproteinemia Type II Details

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