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PCSK9-IN-13

Name: PCSK9-IN-13
Brand: TargetMol
SKU: T73008
Rating: 4.5 (1 reviews)

Catalog No. T73008 Copy Product Info

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PCSK9-IN-13 (compound 3f) is a potent PCSK9 inhibitor with an IC50 of 537 nM. It antagonizes the binding of the low-density lipoprotein receptor (LDLR) to PCSK9 by interacting with a cryptic binding groove on the PCSK9 protein. Since PCSK9 normally mediates the degradation of LDLR, this inhibitor helps maintain higher levels of LDLR on the hepatocyte surface, thereby promoting the uptake of circulating LDL-C. It is a valuable tool for researching novel cholesterol-lowering therapies and cardiovascular disease prevention.

PCSK9-IN-13

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Catalog No. T73008

Cas No. 2244129-23-3

Pack Size	Price	USA Stock	Global Stock
25 mg	$1,670	6-8 weeks	6-8 weeks
50 mg	$2,180	6-8 weeks	6-8 weeks
100 mg	$2,800	6-8 weeks	6-8 weeks

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	PCSK9-IN-13 (compound 3f) is a potent PCSK9 inhibitor with an IC50 of 537 nM. It antagonizes the binding of the low-density lipoprotein receptor (LDLR) to PCSK9 by interacting with a cryptic binding groove on the PCSK9 protein. Since PCSK9 normally mediates the degradation of LDLR, this inhibitor helps maintain higher levels of LDLR on the hepatocyte surface, thereby promoting the uptake of circulating LDL-C. It is a valuable tool for researching novel cholesterol-lowering therapies and cardiovascular disease prevention.
In vitro	PCSK9-IN-13 (0.1-1 uM) blocks PCSK9-LDLR interaction and restores LDL uptake in HepG2 cells [1].
In vivo	Daily s.c. PCSK9-IN-13 (16.4 mg/kg) significantly lowered mouse plasma cholesterol (~10%) [1].

Chemical Properties

Molecular Weight	495.62
Formula	C₃₀H₃₃N₅O₂
Cas No.	2244129-23-3
Smiles	C(C=1C=C(C=C(NC(=O)C2=CC(OC3=CC=CC=C3)=C(C)C=C2)C1)N4C=C(C)N=C4)N5C[C@@H](N)CCC5

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (161.41 mM), Sonication is recommmended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0177 mL	10.0884 mL	20.1767 mL	100.8837 mL
5 mM	0.4035 mL	2.0177 mL	4.0353 mL	20.1767 mL
10 mM	0.2018 mL	1.0088 mL	2.0177 mL	10.0884 mL
20 mM	0.1009 mL	0.5044 mL	1.0088 mL	5.0442 mL
50 mM	0.0404 mL	0.2018 mL	0.4035 mL	2.0177 mL
100 mM	0.0202 mL	0.1009 mL	0.2018 mL	1.0088 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc