产品
编 号：F756680
分子式：C24H26F2N4O2S
分子量：472.55
分子式：C24H26F2N4O2S
分子量：472.55
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CAS No: 2892451-45-3
产品详情
生物活性：
LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 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.
体内研究：
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.Animal Model:CD-1 mice
Dosage:0.5 mg/kg (i.v.) and 5 mg/kg (p.o.)
Administration:Intravenous injection and oral administration
Result:1.19Route of AdministrationIVPO
Dose (mg/kg)0.55
AUCinf (μM*h)0.511.44
Cmax (μM)0.610.60
Tmax (h)0.080.50
T1/2 (h)0.451.46
MRT (h)0.652.35
CL (mL/min)34.3
F (%)28
体外研究：
LRRK2-IN-5 (compound 25; 0-10000 nM; 24 h; HEK293 cells) has excellent potency and GS-LRRK2 selectivity.
LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 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.
体内研究：
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.Animal Model:CD-1 mice
Dosage:0.5 mg/kg (i.v.) and 5 mg/kg (p.o.)
Administration:Intravenous injection and oral administration
Result:1.19Route of AdministrationIVPO
Dose (mg/kg)0.55
AUCinf (μM*h)0.511.44
Cmax (μM)0.610.60
Tmax (h)0.080.50
T1/2 (h)0.451.46
MRT (h)0.652.35
CL (mL/min)34.3
F (%)28
体外研究：
LRRK2-IN-5 (compound 25; 0-10000 nM; 24 h; HEK293 cells) has excellent potency and GS-LRRK2 selectivity.
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