GNE-0877

SKU: orb1226418

Description

GNE-7915 is a highly potent, selective, brain-penetrating LRRK2 inhibitor with Ki of 0.6 nM (LRRK2 G2019S), pLRRK2 cell IC50 of 3 nM; induces abnormal cytoplasmic accumulation of secretory lysosome-related organelles known as lamellar bodies in type II pneumocytes of the lung in nonhuman primates, but no lysosomal abnormality in the kidney.

Key Properties

• CAS Number: 1374828-69-9
• MW: 339.326
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₆F₃N₇
• SMILES: CC(N1N=C(C)C(NC2=NC=C(C(F)(F)F)C(NC)=N2)=C1)(C)C#N
• Target: LRRK2
• Solubility: DMSO: 62 mg/mL (182.7 mM); Ethanol: <1 mg/mL; Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  GNE0877 (10 and 50 mg/kg; i.p. once) inhibits LRRK2 Ser1292 autophosphorylation. Animal model: BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation. Dosage: 10 and 50 mg/kg. Administration: Intraperitoneal injection; 10 and 50 mg/kg once. Result: Tration-dependently inhibited Ser1292 autophosphorylation with an IC50 of 3 nM.
• In Vitro:
  GNE0877 (1 μM; 10-30 min) shows good cellular potency in human liver microsomes and hepatocytes. Cell Viability Assay Cell line: Human liver microsomes and hepatocytes. Concentration: 1 μM. Incubation time: 10, 20 and 30 min. Result: Exibited low turnover and good vitro stability in human liver microsomes and hepatocytes with no glucuronidation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GNE0877

Quick Database Links

Gene Symbol

LRRK2