GNE-0877

Catalog No.S7367 Synonyms: DNL201

For research use only.

GNE-0877 (DNL201) is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 0.7 nM.

GNE-0877 Chemical Structure

CAS No. 1374828-69-9

Selleck's GNE-0877 has been cited by 1 Publication

Purity & Quality Control

Choose Selective LRRK2 Inhibitors

Biological Activity

Description GNE-0877 (DNL201) is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 0.7 nM.
Targets
LRRK2 [1]
0.7 nM(Ki)
In vitro

GNE-0877 significantly inhibits LRRK2 cellular activity with IC50 of 3 nM, and shows low turnover in human liver microsomes and hepatocytes. Besides, GNE-0877 is also a reversible CYP1A2 inhibitor with IC50 of 0.7 μM. [1]

In vivo In vivo, GNE-0877 shows good oral bioavailability and brain penetration. GNE-0877 inhibits in vivo LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation. [1]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation.
  • Dosages: ~50 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 339.32
Formula

C14H16F3N7

CAS No. 1374828-69-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NN(C=C1NC2=NC=C(C(=N2)NC)C(F)(F)F)C(C)(C)C#N

In vivo Formulation Calculator (Clear solution)

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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.

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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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