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PF-06447475

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Catalog No. T2050Cas No. 1527473-33-1

PF-06447475 is a highly effective, specific, brain penetrant LRRK2 inhibitor with IC0 of 3/11 nM for wild type LRRK2 and G2019S LRRK2 respectively.

PF-06447475

PF-06447475

😃Good
Purity: 99.62%
Catalog No. T2050Cas No. 1527473-33-1
PF-06447475 is a highly effective, specific, brain penetrant LRRK2 inhibitor with IC0 of 3/11 nM for wild type LRRK2 and G2019S LRRK2 respectively.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$43In StockIn Stock
10 mg$61In StockIn Stock
25 mg$89In StockIn Stock
50 mg$133In StockIn Stock
100 mg$225In Stock-
200 mg$397InquiryInquiry
1 mL x 10 mM (in DMSO)$48In StockIn 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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Purity:99.62%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
PF-06447475 is a highly effective, specific, brain penetrant LRRK2 inhibitor with IC0 of 3/11 nM for wild type LRRK2 and G2019S LRRK2 respectively.
Targets&IC50
LRRK2 (G2019S):11nM, LRRK2:3nM
In vitro
In the macrophage cell line Raw264.7, PF-06447475 inhibits endogenous LRRK2 kinase activity with IC50 of <10 nM. [2] In astrocytes, PF-06447475 rescues LRRK2 mutation-induced defects in lysosomal morphology and function. [3]
In vivo
In G2019S BAC-transgenic mice, PF-06447475 (100 mg/kg, p.o.) inhibits pS935 and pS1292 phosphorylation of LRRK2 with IC50 of 103 nM and 21 nM, respectively. [1] In G2019S-LRRK2 rats, PF-06447475 (30 mg/kg, p.o.) blocks α-synuclein-induced dopaminergic neurodegeneration and attenuates neuroinflammation associated with G2019S-LRRK2 expression. [2]
Chemical Properties
Molecular Weight305.33
FormulaC17H15N5O
Cas No.1527473-33-1
SmilesN#Cc1cccc(c1)-c1c[nH]c2ncnc(N3CCOCC3)c12
Relative Density.1.40 g/cm3 (Predicted)
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
DMSO: 15.3 mg/mL (50.11 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (8.19 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
1mg5mg10mg50mg
1 mM3.2751 mL16.3757 mL32.7514 mL163.7572 mL
5 mM0.6550 mL3.2751 mL6.5503 mL32.7514 mL
10 mM0.3275 mL1.6376 mL3.2751 mL16.3757 mL
20 mM0.1638 mL0.8188 mL1.6376 mL8.1879 mL
50 mM0.0655 mL0.3275 mL0.6550 mL3.2751 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

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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

Keywords

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