Art. -Nr.: HY-152221

PCSK9-IN-10

Name: PCSK9-IN-10
Brand: MedChemExpress
SKU: HY-152221
Price: 120.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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Based on 1 Customer Validation

PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC₅₀ value of 6.4 µM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia.

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Reinheit : 98.89%
CAS. Nr.: 368434-98-4
Formel: C₁₈H₂₃N₅O₄
Molecular Weight:373.41

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

PCSK9-IN-10 Chemical Structure

CAS. Nr.: 368434-98-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (2)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

PCSK9-IN-10 (compound 3s) (0, 2.5, 5, 12.5, 25 µM; 24 h) significantly decreases the PCSK9 protein expression and increases the expression of LDL receptor (LDLR) in a dose dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Cell Cytotoxicity Assay^[1]

View Protocol

Cell Line:

HepG2 cells
Concentration:

0-1000 µM
Incubation Time:

24 h
Result:

Showed low cytotoxicity to HepG2 cells.

Western Blot Analysis^[1]

View Protocol

Cell Line:

HepG2 cells
Concentration:

0, 2.5, 5, 12.5, 25 µM
Incubation Time:

24 h
Result:

Significantly decreased PCSK9 protein level in a dose dependent manner.

In Vivo

PCSK9-IN-10 (30 mg/kg; p.o.; once a day for 8 weeks) reduces total cholesterol (TC) and atherosclerotic plaque size in ApoE KO mice^[1].

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

Animal Model:

Eight weeks old male ApoE KO mice^[1]
Dosage:

30 mg/kg
Administration:

P.o.; once a day for 8 weeks
Result:

Inhibited both hepatic and serum PCSK9 content obviously and reduced reduced atherosclerotic plaque size.

Chemical Information

CAS. Nr. 368434-98-4
Appearance Solid
Molecular Weight 373.41
Formel C₁₈H₂₃N₅O₄
Color White to off-white
SMILES

O=C(N1C)N(C)C2=C(N(CC3=CC=CC(OC)=C3)C(NCCOC)=N2)C1=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (669.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6780 mL

13.3901 mL

26.7802 mL

5 mM

0.5356 mL

2.6780 mL

5.3560 mL

10 mM

0.2678 mL

1.3390 mL

2.6780 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (5.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (5.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

All Molecular Biology Signal Pathway Related

RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Qiao MQ, et al. Structure-activity relationship and biological evaluation of xanthine derivatives as PCSK9 inhibitors for the treatment of atherosclerosis. Eur J Med Chem. 2022 Dec 26;247:115047. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.6780 mL	13.3901 mL	26.7802 mL	66.9505 mL
	5 mM	0.5356 mL	2.6780 mL	5.3560 mL	13.3901 mL
	10 mM	0.2678 mL	1.3390 mL	2.6780 mL	6.6951 mL
	15 mM	0.1785 mL	0.8927 mL	1.7853 mL	4.4634 mL
	20 mM	0.1339 mL	0.6695 mL	1.3390 mL	3.3475 mL
	25 mM	0.1071 mL	0.5356 mL	1.0712 mL	2.6780 mL
	30 mM	0.0893 mL	0.4463 mL	0.8927 mL	2.2317 mL
	40 mM	0.0670 mL	0.3348 mL	0.6695 mL	1.6738 mL
	50 mM	0.0536 mL	0.2678 mL	0.5356 mL	1.3390 mL
	60 mM	0.0446 mL	0.2232 mL	0.4463 mL	1.1158 mL
	80 mM	0.0335 mL	0.1674 mL	0.3348 mL	0.8369 mL
	100 mM	0.0268 mL	0.1339 mL	0.2678 mL	0.6695 mL

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PCSK9-IN-10