GNE-9605

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GNE-9605 是一种高效、选择性、脑渗透性 LRRK2 抑制剂，Ki 为 2 nM，pLRRK2 IC50 为 19 nM。

GNE-9605 is a highly potent, selective, brain penetrant LRRK2 inhibitor with Ki of 2 nM, pLRRK2 IC50 of 19 nM; dispalys excellent selectivity against 178-membered Invitrogen kinase panel, as well as a representative panel of receptors and ion channels; demonstrates robust concentration-dependent inhibition of LRRK2 Ser1292 autophosphorylation (IC50=20 nM) in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation.

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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%).

GNE9605 | GNE 9605

Autophagy

LRRK2

LRRK2

Neurological Disease

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1536200-31-3

449.8336

C17H20ClF4N7O

>98% (HPLC)

DMSO: ≥ 60 mg/mL

FC(C1=CN=C(NC2=C(Cl)N([C@H]3[C@H](F)CN(C4COC4)CC3)N=C2)N=C1NC)(F)F

2,4-Pyrimidinediamine, N2-[5-chloro-1-[(3R,4R)-3-fluoro-1-(3-oxetanyl)-4-piperidinyl]-1H-pyrazol-4-yl]-N4-methyl-5-(trifluoromethyl)-, rel-

(-20℃)

With Ice Pack

≥ 2 years