产品
编 号：F131874
分子式：C17H20ClN5O3
分子量：377.83
分子式：C17H20ClN5O3
分子量：377.83
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1351758-81-0
产品详情
生物活性：
HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research.
体内研究：
HG-10-102-01 (0-100 mg/kg, IP, once) shows inhibition of LRRK2 Ser910/Ser935 phosphorylation in kidney, spleen, and brain of mice.HG-10-102-01 (1 mg/kg, IV; 10 mg/kg, PO; once) shows good oral bioavailability (%F = 67), a short half-life of 0.13 h, and low plasma exposure.Animal Model:Wild type male C57BL/6 mice
Dosage:0, 3, 10, 30, 50, and 100 mg/kg
Administration:IP, once
Result:Showed near complete dephosphorylation of Ser910 and Ser935 of LRRK2 in all tissues including brain at 100 mg/kg and 50 mg/kg, but only partial inhibition in brain at the 30 and 10 mg/kg doses.
Animal Model:Wild type male C57BL/6 mice
Dosage:1 mg/kg (IV); 10 mg/kg (PO)
Administration:IV, PO; once (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of HG-10-102-01 in male C57BL/6 mice.IV (1 mg/kg) PO (10 mg/kg)
Tmax (h)0.25
Cmax (ng/mL)13301241
AUClast (ng/mL?h)74.85502.34
AUCINF (ng/mL?h)75.06503.41
T1/2 (h)0.13
CL (mL/min/kg)222.04
Vss (L/kg)1.68
F (%)67
体外研究：
HG-10-102-01 (0-3 μM, 90 min) substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant.
HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research.
体内研究：
HG-10-102-01 (0-100 mg/kg, IP, once) shows inhibition of LRRK2 Ser910/Ser935 phosphorylation in kidney, spleen, and brain of mice.HG-10-102-01 (1 mg/kg, IV; 10 mg/kg, PO; once) shows good oral bioavailability (%F = 67), a short half-life of 0.13 h, and low plasma exposure.Animal Model:Wild type male C57BL/6 mice
Dosage:0, 3, 10, 30, 50, and 100 mg/kg
Administration:IP, once
Result:Showed near complete dephosphorylation of Ser910 and Ser935 of LRRK2 in all tissues including brain at 100 mg/kg and 50 mg/kg, but only partial inhibition in brain at the 30 and 10 mg/kg doses.
Animal Model:Wild type male C57BL/6 mice
Dosage:1 mg/kg (IV); 10 mg/kg (PO)
Administration:IV, PO; once (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of HG-10-102-01 in male C57BL/6 mice.IV (1 mg/kg) PO (10 mg/kg)
Tmax (h)0.25
Cmax (ng/mL)13301241
AUClast (ng/mL?h)74.85502.34
AUCINF (ng/mL?h)75.06503.41
T1/2 (h)0.13
CL (mL/min/kg)222.04
Vss (L/kg)1.68
F (%)67
体外研究：
HG-10-102-01 (0-3 μM, 90 min) substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant.
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