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GNE 7915
Axon 2348
CAS:
1351761-44-8
Purity:
99%
- Soluble in DMSO
- MF: C19H21F4N5O3
- MW: 443.4
Description
Highly potent, selective, metabolically stable, and brain-penetrable LRRK2 inhibitor (IC50 value 9 nM for phospho-LRRK2 in vitro). GNE 7915 is selective across 187 screened kinases, and >3200 and 53 times selective over JAK2 and TTK, respectively. GNE 7915 does not suppress LPS-stimulated TNFα and CXCL10 levels in LPS-treated primary wild-type (WT) or knockout (KO) astrocyte cultures, and is not reported to cause cellular or genetic toxicity.
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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