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PCSK9-IN-10

Name: PCSK9-IN-10
Brand: TargetMol
SKU: T72025
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T72025Cas No. 368434-98-4

PCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 µM. By enhancing the expression of Low-Density Lipoprotein Receptor (LDLR) protein and reducing PCSK9 expression, PCSK9-IN-10 effectively decreases atherosclerosis progression. This compound holds promise for hyperlipidemia research applications.

PCSK9-IN-10

🥰Excellent

Purity: 99.06%

Catalog No. T72025Cas No. 368434-98-4

Pack Size	Price	Availability
2 mg	$35	In Stock
5 mg	$58	In Stock
10 mg	$93	In Stock
25 mg	$188	In Stock
50 mg	$296	In Stock
100 mg	$435	In Stock
200 mg	$616	In Stock
1 mL x 10 mM (in DMSO)	$59	In Stock

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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.06%

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	PCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 µM. By enhancing the expression of Low-Density Lipoprotein Receptor (LDLR) protein and reducing PCSK9 expression, PCSK9-IN-10 effectively decreases atherosclerosis progression. This compound holds promise for hyperlipidemia research applications.
Targets&IC50	PCSK9:6.4 µM
In vitro	PCSK9-IN-10 (0, 2.5, 5, 12.5, 25 µM ; 24 h) significantly reduces PCSK9 protein expression and increases the expression of LDL receptor (LDLR) in a dose-dependent manner.[1]
In vivo	PCSK9-IN-10 (30 mg/kg; oral administration; once daily for 8 weeks) reduces total cholesterol (TC) levels and atherosclerotic plaque size in ApoE KO mice.[1]

Chemical Properties

Molecular Weight	373.41
Formula	C₁₈H₂₃N₅O₄
Cas No.	368434-98-4
Smiles	COCCNc1nc2n(C)c(=O)n(C)c(=O)c2n1Cc1cccc(OC)c1
Relative Density.	1.32 g/cm3 (Predicted)
Color	White
Appearance	Solid

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: 225.0 mg/mL (602.6 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (13.39 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6780 mL	13.3901 mL	26.7802 mL	133.9011 mL
5 mM	0.5356 mL	2.6780 mL	5.3560 mL	26.7802 mL
10 mM	0.2678 mL	1.3390 mL	2.6780 mL	13.3901 mL
20 mM	0.1339 mL	0.6695 mL	1.3390 mL	6.6951 mL
50 mM	0.0536 mL	0.2678 mL	0.5356 mL	2.6780 mL
100 mM	0.0268 mL	0.1339 mL	0.2678 mL	1.3390 mL

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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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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

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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