您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Lanabecestat
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Lanabecestat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lanabecestat图片
CAS NO:1383982-64-6
包装与价格:
包装价格(元)
50 mg电议
100 mg电议

产品名称
LY3314814
AZD3293
产品介绍

产品描述

Lanabecestat (AZD3293) is a highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor (Ki: 0.4 nM).

体外活性

Lanabecestat displays a very high target affinity and a markedly slow target off-rate. The off-rate of Lanabecestat has an estimated t1/2 of approximately 9?h. Lanabecestat displays pM potency in primary neuron cultures from mice and guinea pigs and in SH-SY5Y cells over-expressing AβPP (IC50=610 pM, 310 pM, and 80 pM, respectively).

体内活性

In mice, guinea pigs, and dogs, Lanabecestat displays significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ.

细胞实验

Cells are incubated with different Lanabecestat concentrations for 5 to 16?h, and the release of sAβPPβ, Aβ1-40, Aβ1-42, or sAβPPα into the medium is analyzed using kits. Cytotoxic effect of Lanabecestat is evaluated in the cell plates using cell proliferation/cytotoxicity kit.

动物实验

Female 7- to 14-week-old C57BL/6 mice (n=6 per treatment group and time point) receive a vehicle or Lanabecestat solution at 50, 100, or 200 μmol/kg (20, 41, or 82?mg/kg) as a single dose via oral gavage. Mice and guinea pigs are anesthetized 1.5, 2, 3, 4, 6, 8, 16, 24, or 48?h after the (last) administration of vehicle or drug and are then kept under isoflurane anesthesia. Cerebrospinal fluid (CSF) is aspirated from the cisterna magna, and plasma is isolated from blood collected by cardiac puncture into EDTA tubes. The animals are then sacrificed by decapitation, and the brains are dissected into hemispheres.

Cas No.

1383982-64-6

分子式

C26H28N4O

分子量

412.53

别名

LY3314814;AZD3293

储存和溶解度

DMSO:100 mg/mL (242.41 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years