GNE-7915

SKU: orb1307020

Description

GNE-7915 is a potent and selective small molecule inhibitor of LRRK2 kinase with demonstrated brain penetration. It is a valuable research tool for investigating LRRK2's role in Parkinson's disease pathogenesis, enabling both in vitro biochemical assays and in vivo preclinical studies in animal models.

Research Area

Cell Biology

Key Properties

• CAS Number: 1351761-44-8
• MW: 443.4
• Purity: 99.70%
• Formula: C₁₉H₂₁F₄N₅O₃
• SMILES: CCNc1nc(Nc2cc(F)c(cc2OC)C(=O)N2CCOCC2)ncc1C(F)(F)F
• Target: LRRK2
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.51 mM);DMSO:16.67 mg/mL (37.6 mM)

Bioactivity

• Target IC50:
  LRRK2:1 nM(Ki)|LRRK2:9 nM
• In Vivo:
  GNE-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.
• In Vitro:
  BAC transgenic mice expressing human LRRK2 protein wit 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Leucine-rich repeat kinase 2, Inhibitor, GNE-7915, GNE7915, GNE 7915, LRRK2, inhibit

Compound Identifiers

PubChem CID

58539171