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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Autophagy>LRRK2 inhibitors>GNE-7915
GNE-7915
  • GNE-7915

GNE-7915 NEW

Price $39 $56 $116
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: GNE-7915 CAS No.: 1351761-44-8
Purity: ≥95% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameGNE-7915
DescriptionGNE-7915 is a highly potent, selective and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor.
Kinase AssayALK2 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.
In vitroBAC 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 vivoGNE-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.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationH2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 16.67 mg/mL (37.59 mM), Sonication is recommended.
KeywordsLRRK2 | inhibit | Inhibitor | GNE 7915 | Leucine-rich repeat kinase 2 | GNE-7915
Inhibitors RelatedPFE-360 | GNE0877 | CZC-25146 | GSK2578215A | GNE-9605 | CZC-54252 hydrochloride | EB-42486 | LRRK2 inhibitor 1 | LRRK2-IN-7 | LRRK2-IN-1 | CCG-1423 | PF-06454589
Related Compound LibrariesTarget-Focused Phenotypic Screening Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Glutamine Metabolism Compound Library | Anti-Parkinson's Disease Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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