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MRK-560

CAS No. : 677772-84-8

MCE 国际站：MRK-560

产品活性：MRK-560 是一种口服有效的，可渗透血脑屏障的 γ-Secretase 抑制剂，能有效减少大鼠脑和脑脊液中 Aβ 肽。MRK-560 能通过选择性地抑制 PSEN1 来阻碍 NOTCH1 的突变进程。MRK-560 可用于阿尔兹海默病和 T 细胞急性淋巴细胞白血病的研究。

研究领域：Neuronal Signaling  |  Stem Cell/Wnt

作用靶点：γ-secretase

In Vitro: MRK-560 (30, 100, 300, 1000 nM; 15days) blocks mutant NOTCH1 receptor signaling in human T-ALL cell lines.

In Vivo: 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 T_max 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).

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