SML0660

GSK2578215A

≥98% (HPLC)

• 別名: 5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinyl-benzamide
• 実験式（ヒル表記法）: C₂₄H₁₈FN₃O₂
• CAS番号: 1285515-21-0
• 分子量: 399.42
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 色: white to beige
• 溶解性: DMSO: 15 mg/mL, clear
• 保管温度: 2-8°C
• SMILES記法: Fc1nccc(c1)c2cc(c(cc2)OCc4ccccc4)C(=O)Nc3cnccc3
• 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

詳細

生物化学的／生理学的作用

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 is a potent inhibitor of leucine-rich repeat kinase-2 (LRRK2).

GSK2578215A stimulates mitochondrial fragmentation, autophagy and mitophagy.[1]

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable