Atabecestat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Atabecestat (JNJ-54861911) 是一种有效的脑渗透型和具有口服活性 β-位淀粉样蛋白前体蛋白裂解酶 1 (BACE1) 抑制剂，可强力降低脑脊液中的 Aβ 蛋白表达降低。Atabecestat 具有耐受性，并具有持续的药代动力学 (PK) 和药效学 (PD) 特征。Atabecestat 有潜力用于阿尔茨海默氏病的研究。

Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment.

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Atabecestat (100 and 300 mg/kg; p.o. once daily for 3 days) reduces the human Aβ levels in mice.Atabecestat (300 mg/kg; p.o. once) inhibits the exacerbation of vascular abnormalities in APPPS1 mice with 3D6 treatment. Animal Model:5-week-old APPPS1 miceDosage:100 and 300 mg/kg Administration:Oral gavage; 100 and 300 mg/kg; once daily for 3 days Result:Reduced the level of human Aβ1-40 and Aβ1-42 levels in the brain of APPPS1 mice at a dose of 300 mg/kg and resulted in less reduction of human Aβ levels at 24 h with a dose of 100 mg/kg.

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Metabolic Enzyme/Protease

BACE

BACE

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1200493-78-2

367.4

C18H14FN5OS

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (680.46 mM; 超声助溶 )

C[C@]1(C=CSC(N)=N1)c1cc(NC(=O)c2ccc(cn2)C#N)ccc1F

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(-20℃)

With Ice Pack

≥ 2 years