Potent LRRK2 inhibitor (IC50 = 3 nM). Attenuates α-synuclein-induced dopaminergic neurodegeneration and neuroinflammation in G2019S-LRRK2 expressing rats. Also neuroprotective in wild type rats. Brain penetrant.
Sold for research purposes under agreement from Pfizer Inc
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 305.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||6.55 mL||32.75 mL||65.5 mL|
|2.5 mM||1.31 mL||6.55 mL||13.1 mL|
|5 mM||0.66 mL||3.28 mL||6.55 mL|
|25 mM||0.13 mL||0.66 mL||1.31 mL|
References are publications that support the biological activity of the product.
Daher et al (2015) Leucine-rich repeat kinase 2 (LRRK2) pharmacological inhibition abates α-synuclein gene-induced neurodegeneration. J.Biol.Chem. 290 19433 PMID: 26078453
Henderson et al (2015) Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. J.Med.Chem. 58 419 PMID: 25353650
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Literature in this Area
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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.