SML0660

GSK2578215A

≥98% (HPLC)

• Synonym(s): 5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinyl-benzamide
• Empirical Formula (Hill Notation): C₂₄H₁₈FN₃O₂
• CAS Number: 1285515-21-0
• Molecular Weight: 399.42
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 15 mg/mL, clear
• storage temp.: 2-8°C
• InChI: 1S/C24H18FN3O2/c25-23-14-19(10-12-27-23)18-8-9-22(30-16-17-5-2-1-3-6-17)21(13-18)24(29)28-20-7-4-11-26-15-20/h1-15H,16H2,(H,28,29)
• InChI key: WCIGMFCFPXZRMQ-UHFFFAOYSA-N

Description

Biochem/physiol Actions

GSK2578215A is a potent inhibitor of leucine-rich repeat kinase-2 (LRRK2) also known as dardarin or PARK8, a kinase with mutations linked to Parkinson′s disease. Because the most common mutation, G2019S, enhances LRRK2 kinase activity, it is hoped that LRRK2 inhibitors may be useful in treating the disease. GSK2578215A inhibited both wild-type and G2019S mutant LRRK2 kinase activity with IC₅₀s of 10.9 and 8.9 nM respectively. It has good blood-brain barrier (BBB) permeability with a high ratio of brain to plasma distribution in mice.

GSK2578215A stimulates mitochondrial fragmentation, autophagy and mitophagy.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable