GNE-7915

Catalog No.S7528 Batch:S752803

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Technical Data

Formula

C19H21F4N5O3
Molecular Weight 443.40 CAS No. 1351761-44-8
Solubility (25°C)* In vitro DMSO 88 mg/mL (198.46 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 30%PEG300 5%Tween80 60%ddH2O
3.1mg/ml Taking the 1 mL working solution as an example, add 50 μL 62 mg/ml clarified DMSO stock solution to 300 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 600 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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 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]

Protocol (from reference)

Animal Study:[1]
  • 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.

Selleck's GNE-7915 has been cited by 1 publication

LRRK2 deficiency impairs trans-Golgi to lysosome trafficking and endocytic cargo degradation in human renal proximal tubule epithelial cells [ Am J Physiol Renal Physiol, 2018, 315(5):F1465-F1477] PubMed: 30089035

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.