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Background Information:
GNE-7915 is a Blood-Brain Barrier (BBB) penetrablesmall molecule inhibitor of Leucine-Rich Repeat Kinase 2 (LRRK2). It potently (Ki = 1 nM/ IC50 =9 nM (cell Assay)) and selectively (1 out of 187) inhibits the enzyme activity, and is CNS active, metabolically stable (refs 1-2).
Reference:
1. 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 (22), pp 9416–9433.
2. M.E. Kavanagh, et al, Bio.& Med. Chem Letters, 2013, 23 (13) Pages 3690–3696.
APIM050157: GNE-7915
CAS No.: 1351761-44-8.
Molecular Formula: C19H21F4N5O3.
Molecular Weight: 443.4.
Purity: >99.5% (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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