产品
编 号：F203556
分子式：C19H21ClN6O3
分子量：416.86
分子式：C19H21ClN6O3
分子量：416.86
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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2mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1700693-08-8
产品详情
生物活性：
JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome.
体内研究：
JH-II-127 (100 mg/kg; i.p.; single) results in near complete dephosphorylation of Ser935 of LRRK2 in all tissues including brain.1.19Pharmacokinetic Parameters of JH-II-127 in Wild type male C57BL/6 mice.matrixrouteTmax (h)C0/Cmax (ng/mL)AUCLast (h?ng/mL)AUGINF (h?ng/mL)T1/2 (h)CL (mL/min/kg)Vss (L/kg)
plasmaIV (2 mg/kg)-1604.47532.67535.570.6662.241.73
plasmaPO (10 mg/kg)1802.723094.583867.07---
brainIV (2 mg/kg)-1343.6239.31246.470.23135.241.7
brainPO (10 mg/kg)1247.35688.21762.38---
Animal Model:Wild type male C57BL/6 mice.
Dosage:2 mg/kg (for i.v.); 10 mg/kg (for p.o.); 10, 30, 100 mg/kg (for i.p.)
Administration:Intravenous and intraperitoneal injection; oral administration; single.
Result:Led to near complete dephosphorylation of Ser935 of LRRK2 in all tissues including brain when at 100 mg/kg of i.p. and near complete inhibition in all tissues at 30 mg/kg but only partial inhibition in brain at the 10 mg/kg dose.Demonstrated good oral bioavailability.
体外研究：
JH-II-127 (0.03, 0.1, 0.3, 1, 3 μM; 90 min) inhibits LRRK2 in HEK293 cells.JH-II-127 (0.3, 1, 3 μM; 90 min) inhibits endogenously expressed LRRK2 in mouse Swiss 3T3 cells.
JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome.
体内研究：
JH-II-127 (100 mg/kg; i.p.; single) results in near complete dephosphorylation of Ser935 of LRRK2 in all tissues including brain.1.19Pharmacokinetic Parameters of JH-II-127 in Wild type male C57BL/6 mice.matrixrouteTmax (h)C0/Cmax (ng/mL)AUCLast (h?ng/mL)AUGINF (h?ng/mL)T1/2 (h)CL (mL/min/kg)Vss (L/kg)
plasmaIV (2 mg/kg)-1604.47532.67535.570.6662.241.73
plasmaPO (10 mg/kg)1802.723094.583867.07---
brainIV (2 mg/kg)-1343.6239.31246.470.23135.241.7
brainPO (10 mg/kg)1247.35688.21762.38---
Animal Model:Wild type male C57BL/6 mice.
Dosage:2 mg/kg (for i.v.); 10 mg/kg (for p.o.); 10, 30, 100 mg/kg (for i.p.)
Administration:Intravenous and intraperitoneal injection; oral administration; single.
Result:Led to near complete dephosphorylation of Ser935 of LRRK2 in all tissues including brain when at 100 mg/kg of i.p. and near complete inhibition in all tissues at 30 mg/kg but only partial inhibition in brain at the 10 mg/kg dose.Demonstrated good oral bioavailability.
体外研究：
JH-II-127 (0.03, 0.1, 0.3, 1, 3 μM; 90 min) inhibits LRRK2 in HEK293 cells.JH-II-127 (0.3, 1, 3 μM; 90 min) inhibits endogenously expressed LRRK2 in mouse Swiss 3T3 cells.
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