Home Autophagy LRRK2 inhibitor GNE-7915 For research use only.

GNE-7915

GNE-7915 is a highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor, with IC50 and Ki of 9 nM and 1 nM, respectively.

GNE-7915 Chemical Structure

GNE-7915 Chemical Structure

CAS No. 1351761-44-8

Purity & Quality Control

GNE-7915 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells Function assay Inhibition of autophosphorylation of LRRK2 in human HEK293 cells, IC50=0.009 μM 22985112
Click to View More Cell Line Experimental Data

Biological Activity

Description GNE-7915 is a highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor, with IC50 and Ki of 9 nM and 1 nM, respectively.
Targets
LRRK2 [1]
(Cell-free assay)		 LRRK2 [1]
(Cell-free assay)
1 nM(Ki) 9 nM
In vitro
In vitro GNE-7915 is also a moderately potent 5-HT2B antagonist according to in vitro functional assays. GNE-7915 demonstrates excellent in vitro DMPK with minimal turnover in human hepatocytes. [1]
In Vivo
In vivo In rats, GNE-7915 demonstrates excellent in vivo PK profiles with long half-lives, good oral exposure and high passive permeability. GNE-7915 (50 mg/kg i.p. or p.o.) results in concentration-dependent knockdown of pLRRK2 in the brain of BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation. [1]
Animal Research Animal Models BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation
Dosages 50 mg/kg
Administration i.p. ; p.o.

Chemical Information & Solubility

Molecular Weight 443.40 Formula

C19H21F4N5O3
CAS No. 1351761-44-8 SDF Download GNE-7915 SDF
Smiles CCNC1=NC(=NC=C1C(F)(F)F)NC2=C(C=C(C(=C2)F)C(=O)N3CCOCC3)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 22 mg/mL ( (49.61 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy GNE-7915 | GNE-7915 supplier | purchase GNE-7915 | GNE-7915 cost | GNE-7915 manufacturer | order GNE-7915 | GNE-7915 distributor