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Cat. No. M13572
GNE0877 Structure
Size Price Availability Quantity
5mg USD 170  USD170 In stock
10mg USD 275  USD275 In stock
25mg USD 600  USD600 In stock
50mg USD 980  USD980 In stock
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Quality Control & Documentation
Biological Activity

GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM. IC50 value: 3 nM Target: LRRK2 Invitrogen kinase-selectivity profiling(188 kinases) of aminopyrazole GNE0877 at 0.1 μM (145-fold overLRRK2 Ki) resulted in only four kinases showing greater than 50% inhibition (Aurora B = 51%, RSK2 = 52%, RSK4 = 62%, and RSK3 = 68%) and suggested that GNE0877 is a highly selective LRRK2 inhibitor. Furthermore, GNE0877 possessed a 212-fold biochemical-selectivity index over TTK (Ki= 150 nM), which was previously highlighted as an off-target kinase of concern because of the suggested role of TTK in the maintenance of chromosomal stability. The in vivo rat clearance for inhibitor GNE0877 was within 2-fold of measured in vitro stability, and good oral bioavailability (88%) was achieved at 50 mg/kg following administration of a methylcellulose/tween (MCT) suspension.

Chemical Information
Molecular Weight 339.32
CAS Number 1374828-69-9
Solubility (25°C) DMSO 150 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Noeen Malik, et al. Eur J Med Chem. Development and biological evaluation of[ 18 F]FMN3PA & [ 18 F]FMN3PU for leucine-rich repeat kinase 2 (LRRK2) in vivo PET imaging

[2] Isadora Marques Paiva, et al. Prog Neuropsychopharmacol Biol Psychiatry. Inhibition of Lrrk2 reduces ethanol preference in a model of acute exposure in zebrafish

[3] Anthony A Estrada, et al. J Med Chem. Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors

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Keywords: GNE0877 supplier, LRRK2, inhibitors, activators

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