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GNE-7915

Name: GNE-7915
Brand: TargetMol
SKU: T1945
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1945Cas No. 1351761-44-8

Alias GNE7915

GNE-7915 is a highly potent, selective and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor.

GNE-7915

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Purity: 99.89%

Catalog No. T1945Alias GNE7915Cas No. 1351761-44-8

GNE-7915 is a highly potent, selective and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$39	In Stock	In Stock
10 mg	$56	In Stock	In Stock
25 mg	$116	In Stock	In Stock
50 mg	$196	In Stock	In Stock
100 mg	$333	In Stock	In Stock
200 mg	$432	In Stock	In Stock
500 mg	$716	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$43	In Stock	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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Purity:99.89%

Color:White

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Product Introduction

Bioactivity

Description	GNE-7915 is a highly potent, selective and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor.
Targets&IC50	LRRK2:1 nM(Ki), LRRK2:9 nM
In vitro	BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson's disease mutation (PD mutation), exhibit concentration-dependent gene silencing of pLRRK2 in the brain following intraperitoneal injection or oral administration of 50 mg/kg GNE-7915. In rats, GNE-7915 demonstrates favorable pharmacokinetic (PK) properties, including a long half-life, good oral bioavailability, and high passive permeability.
In vivo	GNE-7915 exhibits excellent in vitro pharmacokinetics in human hepatocytes with minimal conversion rates. According to in vitro functional assays, GNE-7915 also acts as a moderately effective antagonist of 5-HT2B.
Kinase Assay	ALK2 kinase assay: Puri?ed recombinant ALK2 proteins, ATP, ATP[γ-32P], and dephosphorylated casein at ?nal concentrations of 2.5 nM, 6 μM, 0.05 μCi/μL , and 0.5 mg/mL, respectively, are aliquoted in kinase bu?er containing 0.2% BSA supplemented with 10 mM MnCl2 into 96-microwell plates, in combination with inhibitor compounds diluted at varying concentrations (0.01 nM to 100 μM). Positive control samples lacking inhibitor compounds, and negative controls lacking recombinant kinase, are also measured. The mixture is reacted at RT for 45 min, quenched with a ?nal concentration of 2% phosphoric acid. The reaction mixture is transferred to 96-well P81 phosphocellulose ?lter plates and bound for 5 min. The plates are washed 20 times with 150 μL of 1% phosphoric acid solution per well by vacuum manifold. Plates are dried at RT for 1 h, sealed, and assayed with Microscint 20 scintillation ?uid using a Spectramax L luminometer. Data is normalized to positive controls at 100% enzyme activity, with negative controls being subtracted as background.
Synonyms	GNE7915

Chemical Properties

Molecular Weight	443.4
Formula	C₁₉H₂₁F₄N₅O₃
Cas No.	1351761-44-8
Smiles	CCNc1nc(Nc2cc(F)c(cc2OC)C(=O)N2CCOCC2)ncc1C(F)(F)F
Relative Density.	1.404 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

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 142.8 mg/mL (322.06 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.51 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	2.2553 mL	11.2765 mL	22.5530 mL	112.7650 mL
5 mM	0.4511 mL	2.2553 mL	4.5106 mL	22.5530 mL
10 mM	0.2255 mL	1.1276 mL	2.2553 mL	11.2765 mL
20 mM	0.1128 mL	0.5638 mL	1.1276 mL	5.6382 mL
50 mM	0.0451 mL	0.2255 mL	0.4511 mL	2.2553 mL
100 mM	0.0226 mL	0.1128 mL	0.2255 mL	1.1276 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