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PF-06446846 hydrochloride

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Catalog No. T16491Cas No. 1632250-50-0

PF-06446846 hydrochloride, an orally active and highly selective inhibitor, targets Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) translation by inducing ribosomal stalling at approximately codon 34, effectively suppressing PCSK9 expression.

PF-06446846 hydrochloride

PF-06446846 hydrochloride

😃Good
Purity: 98.70%
Catalog No. T16491Cas No. 1632250-50-0
PF-06446846 hydrochloride, an orally active and highly selective inhibitor, targets Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) translation by inducing ribosomal stalling at approximately codon 34, effectively suppressing PCSK9 expression.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$52In StockIn Stock
5 mg$123In StockIn Stock
10 mg$208In StockIn Stock
25 mg$496In StockIn Stock
50 mg$745In StockIn Stock
100 mg$1,090-In Stock
200 mg$1,480-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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:98.70%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
PF-06446846 hydrochloride, an orally active and highly selective inhibitor, targets Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) translation by inducing ribosomal stalling at approximately codon 34, effectively suppressing PCSK9 expression.
In vitro
PF-06446846 suppresses the secretion of PCSK9 by Huh7 cells (IC50: 0.3 μM)[1].
In vivo
PF-06446846 (oral gavage; 5-50 mg/kg/day for 14 days) lowers plasma PCSK9 in a dose-dependent manner. It also decreases total cholesterol levels[1].
Chemical Properties
Molecular Weight470.36
FormulaC22H20CIN7O.XHCl
Cas No.1632250-50-0
SmilesCl.Clc1cccnc1N([C@@H]1CCCNC1)C(=O)c1ccc(cc1)-n1nnc2cccnc12
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: 90.00 mg/mL (191.34 mM), Sonication is recommended.
DMSO: 225.00 mg/mL (478.36 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5.00 mg/mL (10.63 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
H2O/DMSO
1mg5mg10mg50mg
1 mM2.1260 mL10.6302 mL21.2603 mL106.3016 mL
5 mM0.4252 mL2.1260 mL4.2521 mL21.2603 mL
10 mM0.2126 mL1.0630 mL2.1260 mL10.6302 mL
20 mM0.1063 mL0.5315 mL1.0630 mL5.3151 mL
50 mM0.0425 mL0.2126 mL0.4252 mL2.1260 mL
100 mM0.0213 mL0.1063 mL0.2126 mL1.0630 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 stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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

Keywords

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