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GNE-9605
LRRK2 inhibitor, brain-penetrant, potent and selective

Catalog No.B4761
Size Price Stock Qty
10mM (in 1mL DMSO)
$160.00
In stock
5mg
$110.00
In stock
25mg
$348.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

Micafungin sodium

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Chemical Properties

Cas No. 1536200-31-3 SDF Download SDF
Chemical Name N2-(5-chloro-1-((3S,4S)-3-fluoro-1-(oxetan-3-yl)piperidin-4-yl)-1H-pyrazol-4-yl)-N4-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
Canonical SMILES CNC1=NC(NC2=C(Cl)N([[email protected]@H]3[[email protected]@H](F)CN(C4COC4)CC3)N=C2)=NC=C1C(F)(F)F
Formula C17H20ClF4N7O M.Wt 449.83
Solubility ≥22.5mg/mL in DMSO Storage Store at -20°C
Physical Appearance A solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

GNE-9605 is a potent and selective inhibitor of LRRK2 with IC50 value of 19 nM [1].

Leucine-rich repeat kinase 2 (LRRK2) is a member of the leucine-rich repeat kinase family. Variants of LRRK2 gene are the most common cause of Parkinson's disease and Crohn's disease.

GNE-9605 is a brain-penetrant, potent and selective LRRK2 inhibitor. GNE-9605 was highly potent against LRRK2 with Ki and IC50 values of 2.0 and 18.7 nM, respectively. In human hepatocytes and liver microsomes, GNE-9605 exhibited excellent human metabolic stability [1].

In rat pharmacokinetic (PK) studies, GNE-9605 exhibited excellent oral bioavailability of 90% and total plasma clearance of 26 mL/min/kg. In bacterial artificial chromosome (BAC) transgenic mice expressing human G2019S LRRK2 protein with the Parkinson’s disease mutation, GNE-9605 (10 or 50 mg/kg) inhibited LRRK2 Ser1292 autophosphorylation with IC50 value of 20 nM in a concentration dependent way. In cynomolgus monkey PK studies, GNE-9605 exhibited excellent brain penetration [1].

Reference:
[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.