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CZC-25146

Name: CZC-25146
Brand: TargetMol
SKU: T3053
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3053Cas No. 1191911-26-8

Alias CHEMBL2397014

CZC-25146 (CHEMBL2397014) is an effective, specific and metabolically stable LRRK2 inhibitor with IC50 of 4.76/6.87 nM for wild-type LRRK2(Leucine-rich repeat kinase-2) and G2019S LRRK2, respectively.

CZC-25146

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Purity: 97.68%

Catalog No. T3053Alias CHEMBL2397014Cas No. 1191911-26-8

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$48	In Stock	In Stock
25 mg	$106	In Stock	In Stock
50 mg	$193	In Stock	In Stock
100 mg	$276	In Stock	In Stock
200 mg	$401	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$31	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:97.68%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

CZC-25146 AI Summary

CZC-25146 shows strong bioactivity as an inhibitor of LRRK2 (Leucine-rich repeat kinase 2) protein. It demonstrated potent inhibition of human recombinant LRRK2 G2019S mutant with an IC50 of 7.0 nM and a Ki of 7.0 nM, and inhibition of human recombinant wild-type LRRK2 with an IC50 of 4.0 nM using biotin-LRRKtide as a substrate, measured via TR-FRET assay. Additionally, it exhibits an EC50 of 4.0 nM in inhibiting LRRK2 G2019S mutant-induced neuronal toxicity in human cortical neurons, and an EC50 of 100.0 nM in rat cortical neurons. In vivo, CZC-25146 shows a drug uptake of 4.0% in the mouse brain at a dose of 1 mg/kg, iv, with a clearance rate of 2.3 mL.min-1.kg-1. These characteristics suggest its potential therapeutic application in diseases involving LRRK2 dysfunction..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	CZC-25146 (CHEMBL2397014) is an effective, specific and metabolically stable LRRK2 inhibitor with IC50 of 4.76/6.87 nM for wild-type LRRK2(Leucine-rich repeat kinase-2) and G2019S LRRK2, respectively.
Targets&IC50	LRRK2 (G2019S):6.87 nM, LRRK2:4.76 nM
Synonyms	CHEMBL2397014

Chemical Properties

Molecular Weight	488.54
Formula	C₂₂H₂₅FN₆O₄S
Cas No.	1191911-26-8
Smiles	COc1cc(ccc1Nc1ncc(F)c(Nc2ccccc2NS(C)(=O)=O)n1)N1CCOCC1
Relative Density.	1.436 g/cm3 (Predicted)

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: 60 mg/mL (122.81 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.09 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	2.0469 mL	10.2346 mL	20.4692 mL	102.3458 mL
5 mM	0.4094 mL	2.0469 mL	4.0938 mL	20.4692 mL
10 mM	0.2047 mL	1.0235 mL	2.0469 mL	10.2346 mL
20 mM	0.1023 mL	0.5117 mL	1.0235 mL	5.1173 mL
50 mM	0.0409 mL	0.2047 mL	0.4094 mL	2.0469 mL
100 mM	0.0205 mL	0.1023 mL	0.2047 mL	1.0235 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:

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