| Bioactivity | GNE0877 is a highly selective, orally active and brain-penetrant LRRK2 inhibitor with an IC50 of 3 nM and a Ki of 0.7 nM. GNE0877 can be used for the research of neuroscience[1]. | ||||||||||||
| Target | IC50: 3 nM (LRRK2) | ||||||||||||
| Invitro | GNE0877 (1 μM; 10-30 min) shows good cellular potency in human liver microsomes and hepatocytes[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | GNE0877 (10 and 50 mg/kg; i.p. once) inhibits LRRK2 Ser1292 autophosphorylation[1]. Animal Model: | ||||||||||||
| Name | GNE0877 | ||||||||||||
| CAS | 1374828-69-9 | ||||||||||||
| Formula | C14H16F3N7 | ||||||||||||
| Molar Mass | 339.32 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Estrada AA, et al. Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem. 2014 Feb 13;57(3):921-36. |