2. Metabolic Enzyme/Protease
  3. PCSK9
  4. PCSK9 degrader 1

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.

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PCSK9 degrader 1 Chemical Structure

PCSK9 degrader 1 Chemical Structure

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1 mg USD 875 In-stock
5 mg USD 1925 In-stock
10 mg USD 3063 In-stock
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Based on 1 publication(s) in Google Scholar

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PCSK9 degrader 1 Related Antibodies

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Description

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[1].

IC50 & Target

Ki: 107 nM (PCSK9)[1]
In Vitro

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.

PCSK9 degrader 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 1.25 μM, 2.5 μM, 5 μM, 10 μM or 20 μM
Incubation Time: 24 hours
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.
Molecular Weight

1077.22

Formula

C53H69FN8O13S
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9283 mL 4.6416 mL 9.2832 mL
5 mM 0.1857 mL 0.9283 mL 1.8566 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.33% ee.: 100.00%

SDS (251 KB)

COA (254 KB) HNMR (304 KB) RP-HPLC (267 KB) NP-HPLC (163 KB) LCMS (103 KB)

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
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
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PCSK9 degrader 1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PCSK9 degrader 1PCSK9Proprotein convertase subtilisin/kexin type 9Inhibitorinhibitorinhibit

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