GNE-0877

Research use only, not for human use.

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.

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.

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.

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.

GNE0877

Autophagy

LRRK2

LRRK2

Neurological Disease

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1374828-69-9

339.326

C14H16F3N7

>98% (HPLC)

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 )

CC(N1N=C(C)C(NC2=NC=C(C(F)(F)F)C(NC)=N2)=C1)(C)C#N

2-methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1H-pyrazol-1-yl)propanenitrile

(-20℃)

With Ice Pack

≥ 2 years