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PCSK9

요약

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

제품 리스트 구매

일부의 생물활성 데이터

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.

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.

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).

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).

사용자 리뷰

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

공개 약품 정보

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

임상 약품 정보

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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