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GNE 7915
- Soluble in DMSO
- MF: C19H21F4N5O3
- MW: 443.4
Description
GNE 7915 is a highly potent, selective, metabolically stable and brain-penetrant LRRK2 inhibitor with an IC50 value of 9 nM for phospho-LRRK2 inhibition in vitro. It shows broad kinase selectivity, including greater than 3200-fold selectivity over JAK2 and 53-fold selectivity over TTK in reported profiling.
LRRK2 kinase activity is strongly linked to genetic and sporadic Parkinson’s disease mechanisms. GNE 7915 is useful for investigating LRRK2 target engagement, CNS kinase pharmacology and neuroinflammation-relevant pathway biology.
Key Features
- Brain-penetrant LRRK2 inhibitor
- IC50: 9 nM for phospho-LRRK2 inhibition
- Selective across broad kinase panels
- Metabolically stable pharmacological profile
Applications
- LRRK2 pharmacology
- Parkinson’s disease model research
- Kinase selectivity profiling
- CNS target-engagement studies
More Information
| Parent CAS No. | 1351761-44-8 |
|---|---|
| Chemical Name | (4-(4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-2-fluoro-5-ethoxyphenyl)(morpholino)methanone |
| SMILES | C(C1=CC(OC)=C(NC2=NC=C(C(F)(F)F)C(NCC)=N2)C=C1F)(N1CCOCC1)=O |
| MFCD | N.A. |
| InChi | InChI=1S/C19H21F4N5O3/c1-3-24-16-12(19(21,22)23)10-25-18(27-16)26-14-9-13(20)11(8-15(14)30-2)17(29)28-4-6-31-7-5-28/h8-10H,3-7H2,1-2H3,(H2,24,25,26,27) |
| InChiKey | XCFLWTZSJYBCPF-UHFFFAOYSA-N |
| CID | 58539171 |
| Short Description | LRRK2 inhibitor |
References
- A.A. Estrada et al. Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J. Med. Chem. 2012, 55, 9416-9433.
- G.C. Luerman et al. Phosphoproteomic evaluation of pharmacological inhibition of leucine-rich repeat kinase 2 reveals significant off-target effects of LRRK-2-IN-1. J. Neurochem. 2014, 128, 561-576.
- M.E. Kavanagh et al. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg. Med. Chem. Lett. 2013, 23, 3690-3696.
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