LRRK2-IN-5 (compound 25) 是一种口服有效的选择性富含亮氨酸重复蛋白激酶 2 基因 (LRRK2) 抑制剂，抑制 GS LRRK2 和 WT LRRK2 的IC50值分别为 1.2 和 16 μM。LRRK2-IN-5 抑制 LRRK2 Ser1292 和 Ser925 的自磷酸化。LRRK2-IN-5 可以通过血脑屏障。

LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC 50 values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier [1].

LRRK2-IN-5 (compound 25; 0-10000 nM; 24 h; HEK293 cells) has excellent potency and GS-LRRK2 selectivity [1]. Cell Viability Assay [1] Cell Line: HEK293 cells Concentration: 0, 30, 100, 300, 1000, 3000, and 10000 nM Incubation Time: 24 hours Result: Reduced GS-LRRK2 pSer935 and GS-LRRK2 pSer1292 autophosphorylation levels over WT-LRRK2.

LRRK2-IN-5 (compound 25; 0.5 mg/kg (i.v.) and 5 mg/kg (p.o.); CD-1 mice) has good pharmacokinetic parametershigh and high bioavailability [1]. Animal Model: CD-1 mice [1] Dosage: 0.5 mg/kg (i.v.) and 5 mg/kg (p.o.) Administration: Intravenous injection and oral administration Result: 1.19 Route of Administration IV PO Dose (mg/kg) 0.5 5 AUC inf (μM*h) 0.51 1.44 C max (μM) 0.61 0.60 T max (h) 0.08 0.50 T 1/2 (h) 0.45 1.46 MRT (h) 0.65 2.35 CL (mL/min) 34.3 F (%) 28

C24H26F2N4O2S

472.55

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years