GNE-9605 Chemical Properties

Boiling point:

587.9±60.0 °C(Predicted)

Density 

1.67±0.1 g/cm3(Predicted)

storage temp. 

Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

solubility 

≥22.5 mg/mL in DMSO

form 

solid

pka

5.04±0.60(Predicted)

GNE-9605 Usage And Synthesis

Description

GNE-9065 is an orally bioavailable and potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC₅₀ = 18.7 nM). It is selective for LRRK2 over 178 kinases, inhibiting only TAK1-TAB1 >50% at a concentration of 0.1 μM. GNE-9065 (10 and 50 mg/kg) inhibits LRRK2 Ser¹²⁹² autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S mutation found in families with autosomal Parkinson’s disease.

References

[1]. estrada aa, chan bk, baker-glenn c, et al. discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (lrrk2) small molecule inhibitors. j med chem, 2014, 57(3): 921-936.

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