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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.
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.
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).
Name | Research Code | Research Phase | Company | First Brand Name | First Approved Country | First Indication | First Approved Company | First Approved Date | Indications | Clinical Trials |
---|---|---|---|---|---|---|---|---|---|---|
Inclisiran sodium | ALN-60212; PCSK9si; ALN-PCSsc; KJX839; KJX-839 | Approved | Alnylam Pharmaceuticals Inc | Leqvio, 乐可为 | EU | Dyslipidemias; Hypercholesterolemia | Novartis Europharm Ltd | 2020-12-09 | Acute Coronary Syndrome; Diabetes Mellitus; Hyperlipidemias; Hyperlipoproteinemia Type II; Cardiovascular Diseases; Dyslipidemias; Coronary Disease; Heterozygous familial hypercholesterolemia; Hypolipoproteinemias; Stroke; Homozygous familial hypercholesterolemia; Kidney Diseases; Coronary Artery Disease; Hypercholesterolemia; Carotid Artery Diseases; Diabetes Mellitus, Type 2; Myocardial Infarction; Atherosclerosis; Plaque, Atherosclerotic | Details |
Evolocumab | AMG-145 | Approved | Amgen Inc, Astellas Pharma Inc | 瑞百安, Repatha | EU | Dyslipidemias; Hypercholesterolemia | Amgen Europe Bv | 2015-07-17 | Acute Coronary Syndrome; Aortic Aneurysm, Abdominal; Diabetes Mellitus; Hyperlipoproteinemia Type II; Hyperlipidemias; Glioma; Rejection in heart transplantation; Cardiovascular Diseases; Coronary Disease; Heterozygous familial hypercholesterolemia; Dyslipidemias; Stroke; HIV Infections; Sepsis; Glioblastoma; Coronary Artery Disease; Hypercholesterolemia; Heart Failure; Atherosclerosis; Myocardial Infarction; Diabetes Mellitus, Type 2; ST Elevation Myocardial Infarction; Homozygous familial hypercholesterolemia | Details |
Tafolecimab | IBI-306 | Approved | Innovent Biologics(Suzhou) Co Ltd | 信必乐 | Mainland China | Dyslipidemias; Hypercholesterolemia | Innovent Biologics(Suzhou) Co Ltd | 2023-08-15 | Homozygous familial hypercholesterolemia; Drug-Related Side Effects and Adverse Reactions; Hypercholesterolemia; Dyslipidemias; Heterozygous familial hypercholesterolemia | Details |
Alirocumab | 316P; REGN-727; SAR-236553 | Approved | Sanofi | 波立达, Praluent | United States | Hypercholesterolemia | Regeneron Pharmaceuticals Inc | 2015-07-24 | Stroke; Hyperlipidemias; Drinking Behavior; Cardiovascular Diseases; Coronary Disease; Vascular Diseases; Heterozygous familial hypercholesterolemia; Dyslipidemias; Acute Coronary Syndrome; Hemorrhage; Intracranial Arteriosclerosis; Angina Pectoris; Shock, Septic; Hypercholesterolemia; Sepsis; ST Elevation Myocardial Infarction; Diabetes Mellitus, Type 2; Atherosclerosis; Myocardial Infarction; Liver Diseases, Alcoholic; HIV Infections; Plaque, Atherosclerotic; Homozygous familial hypercholesterolemia | Details |
Name | Research Code | Research Phase | Company | Indications | Clinical Trials |
---|---|---|---|---|---|
Recombinant human anti-PCSK9 monoclonal antibody (Salubris) | SAL003 | Phase 3 Clinical | Shenzhen Salubris Pharmaceuticals Co Ltd | Hypercholesterolemia; Dyslipidemias; Hyperlipidemias; Hyperlipidemia, Familial Combined | 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 3 Clinical | Merck Sharp & Dohme Corp | Atherosclerosis; Hypercholesterolemia; Kidney Diseases; Cardiovascular Diseases; Arteriosclerosis; Hyperlipoproteinemia Type II | Details |
AZD-8233 | AZD-8233; IONIS-AZ4-2.5-LRx; ION-449 | Phase 2 Clinical | Ionis Pharmaceuticals Inc | Hypercholesterolemia; Dyslipidemias; Hyperlipidemias; Kidney Failure, Chronic | Details |
CiVi-007 | CiVi-007; LNA-PCSK -9; LNA-PCSK9-GalNac | Phase 2 Clinical | F. Hoffmann-La Roche Ltd | Hypercholesterolemia | Details |
CVI-LM-001 | CVI-LM-001; CVI-LM001; C-8304 | Phase 2 Clinical | Xiwei'Ai Medicine Technology (Shanghai) Co Ltd | Hypercholesterolemia; Hyperlipidemias | Details |
ATX-304 | O-304; ATX-304; O-304X | Phase 2 Clinical | Betagenon Ab | Mitochondrial Diseases; Diabetes Mellitus, Type 2; Peripheral Arterial Disease | Details |
MIL-86 | MIL-86 | Phase 2 Clinical | Beijing Mabworks Biotech Co Ltd | Hypercholesterolemia; Heterozygous familial hypercholesterolemia; Cardiovascular Diseases; Hyperlipidemias; 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 |
AZD-0780 | AZD-0780; AZD0780 | Phase 2 Clinical | Dogma Therapeutics | Dyslipidemias; Cardiovascular Diseases | Details |
Recombinant human anti-PCSK9 monoclonal antibody (Tasly Pharm) | B1655; B-1655 | Phase 1 Clinical | Tianjin Tasly Pharmaceutical Co Ltd | Hypercholesterolemia | Details |
DC-371739 | JYP-0739; DC-371739 | Phase 1 Clinical | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Hypercholesterolemia; Dyslipidemias; Hyperlipidemias | Details |
Anti-PCSK9 monoclonal antibody (Biocad) | Phase 1 Clinical | Biocad | Cardiovascular Diseases | Details | |
ATH-04 | ATH-04; Affitope AT04A | Phase 1 Clinical | Affiris Ag | Atherosclerosis | Details |
VERVE-101 | VERVE-101 | Phase 1 Clinical | Broad Institute, Harvard University | Plaque, Atherosclerotic; Hypercholesterolemia; Heterozygous familial hypercholesterolemia | Details |
SAL-092 | SAL092; SAL-092 | Phase 1 Clinical | Shenzhen Salubris Pharmaceuticals Co Ltd | Hypercholesterolemia; Dyslipidemias | Details |
SYH-2053 | SYH2053; SYH-2053 | Phase 1 Clinical | CSPC Pharmaceutical Group Ltd | Hypercholesterolemia; Dyslipidemias; Hyperlipidemia, Familial Combined; Hyperlipidemias | Details |
VERVE-102 | VERVE-102 | Phase 1 Clinical | Verve Therapeutics Inc | Atherosclerosis; Coronary Disease; Heterozygous familial hypercholesterolemia | Details |
SGB-3403 | SGB-3403 | Phase 1 Clinical | Suzhou Sanegene Biopharmaceuticals Ltd | Atherosclerosis; Hypercholesterolemia; Heterozygous familial hypercholesterolemia; Cardiovascular Diseases; Hyperlipidemias | Details |
RN-0191 | RN0191 | Phase 1 Clinical | Rona Therapeutics Inc | Atherosclerosis; Hypercholesterolemia; Dyslipidemias | Details |
RBD-7022 | RBD-7022; RBD7022 | Phase 1 Clinical | Suzhou Ribo Life Science Co Ltd | Hypercholesterolemia; Hyperlipidemias; Hyperlipidemia, Familial Combined | Details |
JX-7002 | JX7002; JX-7002 | Phase 1 Clinical | Zhejiang Jingxin Pharmaceutical Co Ltd | Hypercholesterolemia; Hyperlipidemias | Details |
NN-6434 | NN-6434 | Phase 1 Clinical | Novo Nordisk A/S | Details | |
PCSK9 modulator (Genekey Biotech) | Phase 1 Clinical | Shenzhen Salubris Pharmaceuticals Co Ltd | Metabolic Diseases; Inflammation | Details |
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