| Bioactivity | GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC50 value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) [1]. | ||||||||||||
| In Vivo | GNE-9605 (10 and 50 mg/kg; i.p.; once) inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein[1].GNE-9605 (1 mg/kg, p.o.; 0.5 mg/kg, i.v.; once) displays LRRK2 Ki in the biochemical assay of 2 nM as well as a cellular IC50 of 19 nM. GNE-9605 has a total plasma clearance with excellent oral bioavailability[1]. Animal Model: | ||||||||||||
| Name | GNE-9605 | ||||||||||||
| CAS | 1536200-31-3 | ||||||||||||
| Formula | C17H20ClF4N7O | ||||||||||||
| Molar Mass | 449.83 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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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. [2]. Kumar S, et, al. Exploring the focal role of LRRK2 kinase in Parkinson's disease. Environ Sci Pollut Res Int. 2022 May;29(22):32368-32382. |
GNE-9605
CAS: 1536200-31-3 F: C17H20ClF4N7O W: 449.83
GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC50 value of 18.7
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