GNE-9605
规格
| Cas Number | 1536200-31-3 |
| 规格或纯度 | Moligand™, ≥98% |
| 级别 | Moligand™ |
| 纯度 | ≥98% |
| 包装 | 100mg 或 50mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| Action Type | 抑制剂 |
| Mechanism Of Action | 富亮氨酸重复激酶 2 抑制剂 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 89 mg/mL (197.85 mM); Ethanol: 12 mg/mL warmed with 50ºC Water: bath (26.67 mM); Water: Insoluble; |
| 简短描述 | LRRK2 抑制剂 |
| 英文简短描述 | LRRK2 Inhibitors |
| 过滤标签 | leucine rich repeat kinase 2 Inhibitor,Autophagy,LRRK2 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | GNE-9605 是一种高效、选择性的富亮氨酸重复激酶 2 (LRRK2) 抑制剂，其<sub>Ki</sub>和 IC50 分别为 2 nM 和 19 nM。 |
| 英文描述 |
Information GNE-9605 GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with K i and IC50 of 2 nM and 19 nM, respectively. Targets LRRK2 ; LRRK2 2 nM(Ki); 19 nM In vitro GNE-9605 is highly potent against LRRK2 in both biochemical (Ki = 2.0 nM) and cellular (IC50 = 19 nM) assays. In vitro human MDR1 permeability data, GNE-9605 exhibits excellent brain penetration in higher species. In vivo In vivo rat PK studies with GNE-9605 (1 mg/kg, p.o.) demonstrates a total plasma clearance of 26 mL/min/kg with excellent oral bioavailability (90%). In BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation, GNE-9605 (10 and 50 mg/kg, i.p.) inhibits in vivo LRRK2 Ser1292 autophosphorylation. |