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GNE-9605

Names

[ CAS No. ]:
1536200-31-3

[ Name ]:
GNE-9605

[Synonym ]:
2,4-Pyrimidinediamine, N-[5-chloro-1-[(3S,4S)-3-fluoro-1-(3-oxetanyl)-4-piperidinyl]-1H-pyrazol-4-yl]-N-methyl-5-(trifluoromethyl)-
N-{5-Chloro-1-[(3S,4S)-3-fluoro-1-(3-oxetanyl)-4-piperidinyl]-1H-pyrazol-4-yl}-N-methyl-5-(trifluoromethyl)-2,4-pyrimidinediamine
GNE-9605

Biological Activity

[Description]:

GNE-9605 is a highly potent, selective, and brain-penetrant LRRK2 inhibitor with IC50 of 19 nM.IC50 value:Target: LRRK2GNE-9605 retained excellent predicted human metabolic stability when assayed in human liver microsomes and hepatocytes. Inaddition, no reversible or time-dependent inhibition of any of the major CYP isoforms was observed. The demonstrated metabolic stability, brain penetration across multiple species, and selectivity of these inhibitors support their use in preclinical efficacy and safety studies.

[Related Catalog]:

Signaling Pathways >> Autophagy >> LRRK2
Research Areas >> Neurological Disease

[References]

[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.


[Related Small Molecules]

LRRK2-IN-1 | IKK-16 | MLi-2 | PF-06447475 | GNE7915 | GSK2578215A | CZC-54252 | GNE-0877 | HG-10-102-01 | JH-II-127 | CZC 25146

Chemical & Physical Properties

[ Density]:
1.7±0.1 g/cm3

[ Boiling Point ]:
587.9±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C17H20ClF4N7O

[ Molecular Weight ]:
449.834

[ Flash Point ]:
309.4±32.9 °C

[ Exact Mass ]:
449.135406

[ PSA ]:
80.13000

[ LogP ]:
1.15

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.663

[ Storage condition ]:
2-8℃

Related Compounds