Atabecestat JNJ-54861911,98.76%

产品编号:Bellancom-109052| CAS NO:1200493-78-2| 分子式:C18H14FN5OS| 分子量:367.40

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-109052
4500.00 杭州 北京(现货)
Bellancom-109052
7500.00 杭州 北京(现货)
Bellancom-109052
22500.00 杭州 北京(现货)
Bellancom-109052
35000.00 杭州 北京(现货)

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Atabecestat JNJ-54861911

产品介绍 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。
生物活性

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.

体外研究
体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 5-week-old APPPS1 mice
Dosage: 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.
体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 5-week-old APPPS1 mice
Dosage: 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.
性状Solid
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (680.46 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7218 mL 13.6091 mL 27.2183 mL
5 mM 0.5444 mL 2.7218 mL 5.4437 mL
10 mM 0.2722 mL 1.3609 mL 2.7218 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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