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 |
|---|---|---|---|---|---|---|---|---|---|---|
| Evolocumab | AMG-145 | Approved | Amgen, Astellas | Evolocumab | ema | Amgen Europe B.V. | 2015-07-17 | Stroke, Hyperlipoproteinaemia type IIa, Myocardial infarction (MI), Hypercholesterolemia, Familial hypercholesterolemia, Coronary heart disease | Details | |
| Alirocumab | 316P; REGN-727; SAR-236553 | Approved | Sanofi, Regeneron Pharmaceutical | PRALUENT | fda | Hypercholesterolemia | SANOFI AVENTIS | 2015-07-24 | Hypercholesterolemia | Details |
| Name | Research Code | Research Phase | Company | Indications | Clinical Trials |
|---|---|---|---|---|---|
| PCSK9 modulator (Genekey Biotech) | Phase Ⅰ | Salubris | Inflammation, Metabolic disorders | Details | |
| AK-102 | AK-102,AK102 | Phase Ⅱ | Akeso Biopharma, Yabao Pharmaceutical, Kangrong Oriental (Guangdong) Pharmaceutical | Hyperlipidemia | Details |
| K-312 | K-312,K312 | Phase Ⅰ | Kowa | Dyslipidemia | Details |
| ALN-PCS | ALN-PCS; ALN-PCS01; ALN-PCS02 | Phase Ⅰ | Almac Discovery, The Medicines Company | Hypercholesterolemia | Details |
| SHR-1209 | SHR-1209 | Phase Ⅱ | Jiangsu Hengrui Medicine | Hyperlipidemia, Hypercholesterolemia | Details |
| ATH-06 | ATH-06; AT-06-A | Phase Ⅰ | AFFiRiS | Atherosclerosis | Details |
| Anti-PCSK9 monoclonal antibody (Biocad) | Phase Ⅰ | Biocad | Cardiovascular disorders | Details | |
| SPC-5001 | SPC-5001,SPC5001 | Phase Ⅰ | Roche | Familial hypercholesterolemia | Details |
| BMS-844421 | BMS 844421; BMSPCSK9Rx; BMS-PCSK9; ISIS-405879 | Phase Ⅰ | Ionis Pharmaceuticals, Bristol-Myers Squibb | Hypercholesterolemia | Details |
| Bococizumab | PF-04950615; PF-4950615; RN-316 | Phase Ⅲ | Pfizer | Cardiovascular disorders, Hypercholesterolemia | Details |
| CiVi-007 | CiVi-007; LNA-PCSK -9; LNA-PCSK9-GalNac | Phase Ⅱ | Roche, CiVi Biopharma | Hypercholesterolemia | Details |
| SAL-092 | SAL092; SAL-092 | Phase Ⅰ | Salubris | Mixed dyslipidemia, Hypercholesterolemia | Details |
| MEDI-4166 | MEDI-4166,MEDI4166 | Phase Ⅱ | MedImmune | Cardiovascular disorders, Type 2 diabetes | Details |
| DS-9001 | DS-9001 | Phase Ⅰ | Daiichi Sankyo, Pieris Pharmaceuticals | Dyslipidemia | Details |
| Inclisiran | ALN-60212; ALN-PCSsc; PCSK9si | NDA Filing | Alnylam, The Medicines Company | Atherosclerosis, Familial hypercholesterolemia | Details |
| ATH-04 | ATH-04 | Phase Ⅰ | AFFiRiS | Atherosclerosis | Details |
| Ralpancizumab | PF-05335810; RN 317; PF-5335810 | Phase Ⅰ | Pfizer | Hypercholesterolemia | Details |
| Lodelcizumab | LGT-209; NVP-LGT-209 | Phase Ⅱ | Novartis | Hypercholesterolemia | Details |
| DC-371739 | DC-371739 | Phase Ⅰ | Shanghai Institute of Materia Medica | Hyperlipidemia | Details |
| Recombinant human anti-PCSK9 monoclonal antibody (Tasly Pharm) | Phase Ⅰ | Tasly Pharm | Hyperlipidemia, Hypercholesterolemia | Details | |
| CVI-LM001 | C-8304; CVI-LM001 | Phase Ⅱ | CVI Pharmaceuticals | Hyperlipidemia | Details |
| Frovocimab | LY-3015014 | Phase Ⅱ | Lilly | Hypercholesterolemia | Details |
| LIB-003 | LIB-003 | Phase Ⅲ | LIB Therapeutics | Hypercholesterolemia | Details |
| JS-002 | JS-002,JS002 | Phase Ⅱ | Shanghai Junshi Biosciences | Hypercholesterolemia | Details |
| BMS-962476 | BMS-962476 | Phase Ⅰ | Bristol-Myers Squibb | Hypercholesterolemia | Details |
| IBI-306 | IBI-306 | Phase Ⅲ | Innovent Biologics | Hypercholesterolemia | Details |
| RG-7652 | RG-7652 | Phase Ⅱ | Genentech | Coronary artery disease (CAD), Metabolic disorders, Hyperlipidemia | Details |
| Recombinant human anti-PCSK9 monoclonal antibody (Salubris) | SAL003 | Phase Ⅰ | Salubris | Mixed dyslipidemia, Hypercholesterolemia | Details |
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