Home Autophagy LRRK2 inhibitor GNE-9605 For research use only.

GNE-9605

GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki and IC50 of 2 nM and 19 nM, respectively.

GNE-9605 Chemical Structure

GNE-9605 Chemical Structure

CAS: 1536200-31-3

Purity & Quality Control

Batch: S736801 DMSO] 89 mg/mL] false] Ethanol] 12 mg/mL] false] Water] Insoluble] false Purity: 99.94%
99.94

GNE-9605 Related Products

Choose Selective LRRK2 Inhibitors

Biological Activity

Description GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki and IC50 of 2 nM and 19 nM, respectively.
Targets
LRRK2 [1] LRRK2 [1]
2 nM(Ki) 19 nM
In vitro
In vitro GNE-9605 is highly potent against LRRK2 in both biochemical (Ki = 2.0 nM) and cellular (IC50 = 19 nM) assays. In vitro human MDR1 permeability data, GNE-9605 exhibits excellent brain penetration in higher species. [1]
In Vivo
In vivo In vivo rat PK studies with GNE-9605 (1 mg/kg, p.o.) demonstrates a total plasma clearance of 26 mL/min/kg with excellent oral bioavailability (90%). In BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation, GNE-9605 (10 and 50 mg/kg, i.p.) inhibits in vivo LRRK2 Ser1292 autophosphorylation. [1]
Animal Research Animal Models G2019S LRRK2 transgenic mice
Dosages 10, 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 449.83 Formula

C17H20ClF4N7O
CAS No. 1536200-31-3 SDF Download GNE-9605 SDF
Smiles CNC1=NC(=NC=C1C(F)(F)F)NC2=C(N(N=C2)C3CCN(CC3F)C4COC4)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (197.85 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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

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