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PCSK9

概要

Name:Proprotein convertase subtilisin kexin type 9
Target Synonym:EC 3.4.21,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 Preproprotein,Hypercholesterolemia, Autosomal Dominant 3,EC 3.4.21.-,HCHOLA3,LDLCQ1,FH3,EC 3.4.21.111,Neural Apoptosis Regulated Convertase 1,FHCL3
Number of Launched Drugs:4
Number of Drugs in Clinical Trials:27
Lastest Research Phase:Approved

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製造番号 種類 製品説明 構造 純度 特徴
CEA-C202 Human ClinMax™ Human PCSK9 ELISA Kit
PC9-H52H7 Human Human PCSK9 Protein, His Tag
PC9-H52H7-structure
PC9-H52H7-sds
EP-103 Human PCSK9 [Biotinylated] : LDL R Inhibitor Screening ELISA Assay Pair
PC9-H5256 Human Human PCSK9 Protein, Fc Tag
PC9-H5256-structure
PC9-H5256-sds
PC9-H52E4 Hamster Hamster PCSK9 Protein, His Tag
PC9-H52E4-structure
PC9-H52E4-sds
PC9-C5223 Cynomolgus Cynomolgus PCSK9 Protein, His Tag
PC9-C5223-structure
PC9-C5223-sds
PC9-M82E1 Mouse Biotinylated Mouse PCSK9 Protein, Avitag™,His Tag
PC9-M82E1-structure
PC9-M82E1-sds
PCY-H5225 Human Human PCSK9 (D374Y) Protein, His Tag (MALS verified)
PCY-H5225-structure
PCY-H5225-sds
PC9-C52H2 Rhesus macaque Rhesus macaque PCSK9 Protein, His Tag
PC9-C52H2-structure
PC9-C52H2-sds
PC9-R52H4 Rat Rat PCSK9 Protein, His Tag
PC9-R52H4-structure
PC9-R52H4-sds
PCY-H82E7 Human Biotinylated Human PCSK9 (D374Y) Protein, Avitag™,His Tag
PCY-H82E7-structure
PCY-H82E7-sds
PC9-H82E7 Human Biotinylated Human PCSK9 Protein, Avitag™,His Tag (MALS verified)
PC9-H82E7-structure
PC9-H82E7-sds
PC9-M5228 Mouse Mouse PCSK9 Protein, His Tag
PC9-M5228-structure
PC9-M5228-sds
PC9-H5223 Human Human PCSK9 Protein, His Tag (MALS Verified)
PC9-H5223-structure
PC9-H5223-sds
ACRO Quality

生物活性データの一部

PCY-H5225-Cell-based assay
PCSK9 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.

Protocol
PCY-H5225-Cell-based assay
PCSK9 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.

Protocol
PC9-H5256-BLI
PCSK9 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).

Protocol
PC9-H52E4-BLI
PCSK9 BLI

Loaded Human LDL R, Fc Tag 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).

Protocol

カスタマーレビュー

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

相関分子

LDL R

公開薬物情報

Name Research Code Research Phase Company First Brand Name First Approved Country First Indication First Approved Company First Approved Date Indications Clinical Trials
Evolocumab AMG-145 Approved Amgen Inc, Astellas Pharma Inc 瑞百安, Repatha Mainland China Atherosclerosis; Homozygous familial hypercholesterolemia Amgen Inc 2015-07-17 Acute Coronary Syndrome; Hyperlipoproteinemia Type II; Diabetes Mellitus; Hyperlipidemias; Glioma; Rejection in heart transplantation; Cardiovascular Diseases; Coronary Disease; Dyslipidemias; Heterozygous familial hypercholesterolemia; Stroke; Homozygous familial hypercholesterolemia; Sepsis; Glioblastoma; Coronary Artery Disease; Hypercholesterolemia; Atherosclerosis; Diabetes Mellitus, Type 2; Myocardial Infarction; Heart Failure; HIV Infections Details
Alirocumab 316P; REGN-727; SAR-236553 Approved Sanofi, Regeneron Pharmaceuticals Inc 波立达, Praluent Mainland China Dyslipidemias; Hypercholesterolemia; Atherosclerosis Sanofi-Aventis Groupe 2015-07-24 Acute Coronary Syndrome; Hyperlipidemias; Drinking Behavior; Cardiovascular Diseases; Vascular Diseases; Coronary Disease; Dyslipidemias; Heterozygous familial hypercholesterolemia; Hemorrhage; Stroke; Intracranial Arteriosclerosis; Homozygous familial hypercholesterolemia; Sepsis; Hypercholesterolemia; ST Elevation Myocardial Infarction; Diabetes Mellitus, Type 2; Atherosclerosis; Liver Diseases, Alcoholic; Plaque, Atherosclerotic; HIV Infections; Shock, Septic Details
Inclisiran sodium ALN-60212; PCSK9si; ALN-PCSsc; KJX839; KJX-839 Approved Alnylam Pharmaceuticals Inc Leqvio United States Heterozygous familial hypercholesterolemia; Atherosclerosis Novartis Pharma Ag 2020-12-09 Plaque, Atherosclerotic; Homozygous familial hypercholesterolemia; Atherosclerosis; Diabetes Mellitus, Type 2; Hypercholesterolemia; Kidney Diseases; Coronary Artery Disease; Acute Coronary Syndrome; Hypolipoproteinemias; Heterozygous familial hypercholesterolemia; Coronary Disease; Dyslipidemias; Cardiovascular Diseases; Hyperlipoproteinemia Type II; Diabetes Mellitus; Hyperlipidemias Details

臨床試験情報

Name Research Code Research Phase Company Indications Clinical Trials
Recombinant human anti-PCSK9 monoclonal antibody (Tasly Pharm) B1655; B-1655 Phase 1 Clinical Tianjin Tasly Pharmaceutical Co Ltd Hypercholesterolemia Details
PCSK9 modulator (Genekey Biotech) Phase 1 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Metabolic Diseases; Inflammation Details
SAL-092 SAL092; SAL-092 Phase 1 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Hypercholesterolemia; Dyslipidemias Details
NN-6434 NN-6434 Phase 1 Clinical Novo Nordisk A/S Details
Anti-PCSK9 monoclonal antibody (Biocad) Phase 1 Clinical Biocad Cardiovascular Diseases Details
Lodelcizumab LGT-209; NVP-LGT-209 Novartis Pharma Ag Details
Recaticimab SHR-1209 Phase 3 Clinical Jiangsu Hengrui Medicine Co Ltd Hypercholesterolemia; Hyperlipidemias Details
MEDI-4166 MEDI-4166 Medimmune Llc Details
BMS-844421 BMS-PCSK9; BMS 844421; BMSPCSK9Rx; ISIS-405879 Ionis Pharmaceuticals Inc Details
K-312 K-312 Kowa Co Ltd Details
DC-371739 DC-371739 Phase 1 Clinical Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Hypercholesterolemia; Dyslipidemias Details
Ralpancizumab RN 317; PF-5335810; PF-05335810 Pfizer Pharmaceuticals Ltd (China) Details
CVI-LM-001 CVI-LM-001; CVI-LM001; C-8304 Phase 2 Clinical Xiwei'Ai Medicine Technology (Shanghai) Co Ltd Hypercholesterolemia; Hyperlipidemias Details
Ebronucimab AK-102 Phase 3 Clinical Zhongshan Akeso Biopharma Co Ltd, Yabao Us Pharmaceutical Co Ltd Homozygous familial hypercholesterolemia; Hypercholesterolemia; Heterozygous familial hypercholesterolemia; Hyperlipidemias; Hyperlipoproteinemia Type II; Hyperlipidemia, Familial Combined Details
MIL-86 MIL-86 Phase 2 Clinical Beijing Mabworks Biotech Co Ltd Hypercholesterolemia; Heterozygous familial hypercholesterolemia; Cardiovascular Diseases; Hyperlipidemias; Hyperlipoproteinemia Type II Details
VERVE-101 VERVE-101 Phase 1 Clinical Broad Institute, Harvard University Plaque, Atherosclerotic; Hypercholesterolemia; Heterozygous familial hypercholesterolemia Details
Recombinant human anti-PCSK9 monoclonal antibody (Salubris) SAL003 Phase 1 Clinical Shenzhen Salubris Pharmaceuticals Co Ltd Hypercholesterolemia; Dyslipidemias; Hyperlipidemia, Familial Combined Details
RBD-7022 RBD-7022; RBD7022 Phase 1 Clinical Suzhou Ruibo Biological Technology Co Ltd Hypercholesterolemia; Hyperlipidemias Details
AZD-8233 AZD-8233; IONIS-AZ4-2.5-LRx; ION-449 Phase 2 Clinical Ionis Pharmaceuticals Inc Hypercholesterolemia; Dyslipidemias; Kidney Failure, Chronic; Hyperlipidemias Details
AZD-0780 AZD0780; AZD-0780 Phase 1 Clinical Astrazeneca Plc Dyslipidemias Details
Lerodalcibep LIB-003 Phase 3 Clinical Lib Therapeutics Llc Atherosclerosis; Hypercholesterolemia; Stroke; Heterozygous familial hypercholesterolemia; Cardiovascular Diseases; Arteriosclerosis; Hyperlipoproteinemia Type II Details
MK-0616 MK-0616 Phase 2 Clinical Merck Sharp & Dohme Corp Atherosclerosis; Hypercholesterolemia; Kidney Diseases; Hyperlipoproteinemia Type II Details
NNC0385-0434 NNC0385-0434 Phase 2 Clinical Novo Nordisk A/S Plaque, Atherosclerotic; Diabetes Mellitus, Type 2; Hypercholesterolemia; Cardiovascular Diseases; Renal Insufficiency, Chronic; Arteriosclerosis Details
Ongericimab JS-002 Phase 3 Clinical Shanghai Junshi Biosciences Co Ltd Hypertriglyceridemia; Atherosclerosis; Hypercholesterolemia; Neoplasms; Dyslipidemias; Heterozygous familial hypercholesterolemia; Hyperlipidemias; Hyperlipidemia, Familial Combined Details
ATH-04 ATH-04 Phase 1 Clinical Affiris Ag Atherosclerosis Details

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