产品
编 号：F423942
分子式：C19H17ClF5NO4S2
分子量：517.92
分子式：C19H17ClF5NO4S2
分子量：517.92
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
结构图
CAS No: 677772-84-8
产品详情
生物活性：
MRK-560 is an orally active, brain barrier-penetrating γ-Secretase inhibitor, can potently reduces Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 also decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL).
体内研究：
MRK-560 (15.54 mg/kg; S.C.; single daily for 14 days) shows strong antileukemic effects on T-ALL model.MRK-560 (1, 3, 10, 30, 100 mg/kg; p.o.; single) shows good blood-brain barrier permeability in a dose-dependent manner in rats.MRK-560 (1, 3, 10, 30, 100 mg/kg; p.o.; single) inhibits the production of Aβ levels in brain and cerebrospinal fluid.MRK-560 (1 mg/kg; p.o.; single) shows a good bioavailability of 70 to 90%, and Tmax is 12 h.MRK-560 (1 mg/kg; i.v.; single) is suitable for once-a-day dosing (with a low plasma clearance and a half-life of more than 15 h).Animal Model:Tg (HLA-DRB1) 31Dmz/Szj (NSG) mice (T-ALL (T cell acute lymphoblastic leukemia) model).
Dosage:15.54 mg/kg
Administration:Subcutaneous injection; single daily for 14 days.
Result:Resulted in strong antileukemic effects and improved median survival to 30 days compared to 18 days in vehicle-treated mice.
Animal Model:Male Sprague-Dawley rats (250-300 g).
Dosage:1, 3, 10, 30, 100 mg/kg
Administration:Oral administration; single (experiment is performed 8 h later)
Result:Increased the plasma and brain concentrations in a dose-dependent manner.Reduced (dose-dependent) both brain and CSF Aβ levels, with essentially complete inhibition of the production of both peptides being observed at a dose of 100 mg/kg.
Animal Model:Male Sprague-Dawley rats (250-300 g).
Dosage:1 mg/kg
Administration:Intravenously and orally administration; single.
Result:Showed Tmax after the oral dose was 12 h,and bioavailability was 70 to 90%.Revealed a low plasma clearance of less than 5 mL/min/kg with a volume of distribution of approximately 6 L/kg, which translated to a long half-life of more than 15 h.
体外研究：
MRK-560 (30, 100, 300, 1000 nM; 15days) blocks mutant NOTCH1 receptor signaling in human T-ALL cell lines.
MRK-560 is an orally active, brain barrier-penetrating γ-Secretase inhibitor, can potently reduces Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 also decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL).
体内研究：
MRK-560 (15.54 mg/kg; S.C.; single daily for 14 days) shows strong antileukemic effects on T-ALL model.MRK-560 (1, 3, 10, 30, 100 mg/kg; p.o.; single) shows good blood-brain barrier permeability in a dose-dependent manner in rats.MRK-560 (1, 3, 10, 30, 100 mg/kg; p.o.; single) inhibits the production of Aβ levels in brain and cerebrospinal fluid.MRK-560 (1 mg/kg; p.o.; single) shows a good bioavailability of 70 to 90%, and Tmax is 12 h.MRK-560 (1 mg/kg; i.v.; single) is suitable for once-a-day dosing (with a low plasma clearance and a half-life of more than 15 h).Animal Model:Tg (HLA-DRB1) 31Dmz/Szj (NSG) mice (T-ALL (T cell acute lymphoblastic leukemia) model).
Dosage:15.54 mg/kg
Administration:Subcutaneous injection; single daily for 14 days.
Result:Resulted in strong antileukemic effects and improved median survival to 30 days compared to 18 days in vehicle-treated mice.
Animal Model:Male Sprague-Dawley rats (250-300 g).
Dosage:1, 3, 10, 30, 100 mg/kg
Administration:Oral administration; single (experiment is performed 8 h later)
Result:Increased the plasma and brain concentrations in a dose-dependent manner.Reduced (dose-dependent) both brain and CSF Aβ levels, with essentially complete inhibition of the production of both peptides being observed at a dose of 100 mg/kg.
Animal Model:Male Sprague-Dawley rats (250-300 g).
Dosage:1 mg/kg
Administration:Intravenously and orally administration; single.
Result:Showed Tmax after the oral dose was 12 h,and bioavailability was 70 to 90%.Revealed a low plasma clearance of less than 5 mL/min/kg with a volume of distribution of approximately 6 L/kg, which translated to a long half-life of more than 15 h.
体外研究：
MRK-560 (30, 100, 300, 1000 nM; 15days) blocks mutant NOTCH1 receptor signaling in human T-ALL cell lines.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备