产品
编 号:F181685
分子式:C17H20ClF4N7O
分子量:449.83
产品类型
结构图
CAS No: 1536200-31-3
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产品详情
生物活性:
GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC50 value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) .
体内研究:
GNE-9605 (10 and 50 mg/kg; i.p.; once) inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein.GNE-9605 (1 mg/kg, p.o.; 0.5 mg/kg, i.v.; once) displays LRRK2 Ki in the biochemical assay of 2 nM as well as a cellular IC50 of 19 nM. GNE-9605 has a total plasma clearance with excellent oral bioavailability. Animal Model:BAC transgenic mice expressing human LRRK2 protein.
Dosage:10 and 50 mg/kg
Administration:Intraperitoneal injection; once
Result:Inhibited LRRK2 Ser1292 autophosphorylation in a dose-dependent manner.
Animal Model:BAC transgenic mice expressing human LRRK2 protein.
Dosage:1 mg/kg, p.o.; 0.5 mg/kg, i.v.
Administration:Oral administration and intravenous injection; once
Result:Demonstrated a total plasma clearance of 26 mL min-1 kg-1 with excellent oral bioavailability (90%).