Potent leucine-rich repeat kinase 2 (LRRK2) inhibitor (IC50 values are 8.9 and 10.1nm respectively for LRRK2[G2019S] mutant and wild-type LRRK2 respectively). Displays selectivity for LRRK2 against a panel of 460 other kinases. Blocks Ser910 and Ser935 phosphorylation in vitro and in peripheral tissues in vivo. Brain penetrant.TLC Conditions:Rf = 0.7 (Dichloromethane:Methanol:Ammonia soln. [90:9:1])Method for Determining Identity:Proton NMR Spectroscopic Analysis and Mass Spectrum AnalysisElemental Analysis:Calculated: %C: 72.17, %H: 4.54, %N: 10.52Solubility:GSK2578215A is supplied as a crystalline solid. A stock solution may be made by dissolving the GSK2578215A in the solvent of choice. GSK2578215A is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of GSK2578215A in ethanol is approximately 1 mg/ml and approximately 10mg/ml in DMSO and DMF.GSK2578215A is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, GSK2578215A should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. GSK2578215A has a solubility of approximately 0.5mg/ml in a 1:1 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.Storage and Stability:Stored at RT. Stable for 6 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap..
