PCSK9 degrader 1
Based on 1 Customer Validation
PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor.
For research use only. We do not sell to patients.
- Purity: 98.33%
- Formula: C53H69FN8O13S
- Molecular Weight:1077.22
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Ki: 107 nM (PCSK9)[1]
PCSK9 degrader 1 (Compound 16; 1.25-20 μM; 24 hours; HEK293 cells) treatment shows a clear concentration-dependent degradation of both the pro and mature form of PCSK9 yielding a half-maximal degradation concentration of 4.8 and 3.4 μM, as well as a maximum percentage of degradation at 20 μM of 58% and 61%, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:1.25 μM, 2.5 μM, 5 μM, 10 μM or 20 μM
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Incubation Time:24 hours
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Result:Showed a clear concentration-dependent degradation of both the pro and mature form of PCSK9 yielding a half-maximal degradation concentration of 4.8 and 3.4 μM, as well as a maximum percentage of degradation at 20 μM of 58% and 61%, respectively.
Chemical Information
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Appearance Solid
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Molecular Weight 1077.22
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Formula C53H69FN8O13S
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Color White to off-white
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SMILES
OC(C(C=C1)=CC=C1C(C(F)=C2)=CC=C2OC(C(OCCOCCNC([C@@H](NC(OC(C)(C)C)=O)CCCN/C(NC(OC(C)(C)C)=O)=N/C(OC(C)(C)C)=O)=O)=C3)=CC4=C3CCN[C@]4(C)CC(NC5=NC=CS5)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (92.83 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.9283 mL | 4.6416 mL | 9.2832 mL | 23.2079 mL |
| 5 mM | 0.1857 mL | 0.9283 mL | 1.8566 mL | 4.6416 mL | |
| 10 mM | 0.0928 mL | 0.4642 mL | 0.9283 mL | 2.3208 mL | |
| 15 mM | 0.0619 mL | 0.3094 mL | 0.6189 mL | 1.5472 mL | |
| 20 mM | 0.0464 mL | 0.2321 mL | 0.4642 mL | 1.1604 mL | |
| 25 mM | 0.0371 mL | 0.1857 mL | 0.3713 mL | 0.9283 mL | |
| 30 mM | 0.0309 mL | 0.1547 mL | 0.3094 mL | 0.7736 mL | |
| 40 mM | 0.0232 mL | 0.1160 mL | 0.2321 mL | 0.5802 mL | |
| 50 mM | 0.0186 mL | 0.0928 mL | 0.1857 mL | 0.4642 mL | |
| 60 mM | 0.0155 mL | 0.0774 mL | 0.1547 mL | 0.3868 mL | |
| 80 mM | 0.0116 mL | 0.0580 mL | 0.1160 mL | 0.2901 mL |
PCSK9 degrader 1 Related Classifications
HY-130245 Related Classifications
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