SML0660

GSK2578215A

≥98% (HPLC)

• Synonym(e): 5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinyl-benzamide
• Empirische Formel (Hill-System): C₂₄H₁₈FN₃O₂
• CAS-Nummer: 1285515-21-0
• Molekulargewicht: 399.42
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 15 mg/mL, clear
• Lagertemp.: 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)
• InChIKey: WCIGMFCFPXZRMQ-UHFFFAOYSA-N

Beschreibung

Biochem./physiol. Wirkung

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.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable