2. Metabolic Enzyme/Protease
  3. PCSK9
  4. PCSK9-IN-13

PCSK9-IN-13(compound 3f) is a potent PCSK9 inhibitor, which can antagonize low-density lipoprotein (LDL) receptor binding by binding to PCSK9, with an IC50 of 537 nM.

For research use only. We do not sell to patients.

PCSK9-IN-13 Chemical Structure

PCSK9-IN-13 Chemical Structure

CAS No. : 2244129-23-3

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5 mg USD 425 In-stock
10 mg USD 680 In-stock
25 mg USD 1360 In-stock
50 mg USD 2200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PCSK9-IN-13 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PCSK9-IN-13(compound 3f) is a potent PCSK9 inhibitor, which can antagonize low-density lipoprotein (LDL) receptor binding by binding to PCSK9, with an IC50 of 537 nM[1].

Cellular Effect
Cell Line Type Value Description References
Sf21 IC50
> 10 μM
Compound: 3f
Inhibition of recombinant human N-terminal GST-tagged c-Kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using FAM-labelled P22 peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1
Inhibition of recombinant human N-terminal GST-tagged c-Kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using FAM-labelled P22 peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1
[PMID: 32051094]
In Vitro

PCSK9-IN-13(compound 3f) (0.1 or 1 μM) restores LDL uptake in HepG2 hepatocytes in a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PCSK9-IN-13 Related Antibodies
In Vivo

PCSK9-IN-13(compound 3f) (3.28 or 16.4 mg/kg/day, s.c., 14 days) in male C57BL/6 mice dose not show a reduction in total cholesterol at a dose of 3.28 mg/kg, however, a dose of 16.4 mg/kg shows a significant reduction of total cholesterol plasma levels by approximately 10%, and exhibits excellent bioavailability[1].
The pharmacokinetic parameters of PCSK9-IN-13(compound 3f) in C57BL/6 mice

Parameter SC PO IV(single) IV(cassette)
Dose(mg/kg) 20 20 5 0.4
Tmax(h) 1 2 - -
Cmax(ng/mL) 2207 52.6 - -
CL(L/h/kg) - - 1.09 0.3
Vss(L/kg) - - 3.87 9.13
T1/2(h) 5.47 - 9.86 25.7
AUC∞(h*ng/mL) 16811 - 4605 1472
MRT∞(h) - - 3.56 34.9
F(%) 91.3 0.527 - -

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

495.62

Formula

C30H33N5O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC(OC2=CC=CC=C2)=C(C=C1)C)NC3=CC(N4C=C(N=C4)C)=CC(CN5C[C@H](CCC5)N)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (201.77 mM; Need ultrasonic; 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 2.0177 mL 10.0884 mL 20.1767 mL
5 mM 0.4035 mL 2.0177 mL 4.0353 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)

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.04 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.04 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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 2.0177 mL 10.0884 mL 20.1767 mL 50.4419 mL
5 mM 0.4035 mL 2.0177 mL 4.0353 mL 10.0884 mL
10 mM 0.2018 mL 1.0088 mL 2.0177 mL 5.0442 mL
15 mM 0.1345 mL 0.6726 mL 1.3451 mL 3.3628 mL
20 mM 0.1009 mL 0.5044 mL 1.0088 mL 2.5221 mL
25 mM 0.0807 mL 0.4035 mL 0.8071 mL 2.0177 mL
30 mM 0.0673 mL 0.3363 mL 0.6726 mL 1.6814 mL
40 mM 0.0504 mL 0.2522 mL 0.5044 mL 1.2610 mL
50 mM 0.0404 mL 0.2018 mL 0.4035 mL 1.0088 mL
60 mM 0.0336 mL 0.1681 mL 0.3363 mL 0.8407 mL
80 mM 0.0252 mL 0.1261 mL 0.2522 mL 0.6305 mL
100 mM 0.0202 mL 0.1009 mL 0.2018 mL 0.5044 mL
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PCSK9-IN-13 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-IN-132244129-23-3PCSK9Proprotein convertase subtilisin/kexin type 9LDLinteractionInhibitorinhibitorinhibit

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