GNE-9605

Catalog No.S7368

For research use only.

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

CAS No. 1536200-31-3

Purity & Quality Control

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

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 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]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: G2019S LRRK2 transgenic mice
  • Dosages: 10, 50 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 89 mg/mL
(197.85 mM)
Ethanol 12 mg/mL warmed
(26.67 mM)
Water Insoluble

Chemical Information

Molecular Weight 449.83
Formula

C17H20ClF4N7O

CAS No. 1536200-31-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CNC1=NC(=NC=C1C(F)(F)F)NC2=C(N(N=C2)C3CCN(CC3F)C4COC4)Cl

In vivo Formulation Calculator (Clear solution)

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

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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.

Molarity Calculator

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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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