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 > ANA-12
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:
 
ANA-12
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。
ANA-12图片
CAS NO:219766-25-3
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
ANA 12
ANA12
产品介绍
ANA-12 是一种选择性TrkB拮抗剂,对高亲和力和低亲和力位点的IC50分别为45.6 nM和41.1 μM。

产品描述

ANA-12 is a potent and selective TrkB antagonist with anxiolytic and antidepressant activity in mice.

体外活性

在雄性Sprague-Dawley大鼠中,ANA-12(3 μg/次)阻断内侧核孤束核(mNTS)BDNF对减少食物摄入的作用.在雄性C57BL/6小鼠中,ANA-12(0.5 mg/kg,腹膜内)显示对脂多糖诱导的抑郁样行为的抗抑郁作用.在雄性野生型小鼠中,ANA-12逆转乙醇摄入并诱导D3受体下调,但在D3R -/- 小鼠中无效.

体内活性

在nnr5 PC12-TrkB细胞中,ANA-12在低至10 nM的浓度下阻止脑源性神经营养因子(BDNF)诱导的神经突生长。ANA-12可选择性直接与TrkB受体结合,抑制TrkB下游通路,而不改变TrkA和TrkC功能。ANA-12在DRG神经元中,消除了BDNF对增加内向电流的作用。

激酶实验

ANA-12 Binding assay: Maxisorp ELISA 96-well plates are coated with various concentrations of Trk BECD -Fc, 20 mg/ml BSA, or 1 mg/mL IgG-Fc (polyclonal anti-TrkB) in a carbonate buffer (pH 9.6) overnight at 4°C. Plates are saturated with 0.5% BSA in PBS for 2 hours at room temperature and extensively washed in PBS-Tween 0.05%. Bodipy–ANA-12 is then incubated in 0.5% PBS-BSA for 1 hour at room temperature before the addition of BDNF in 0.5% PBS-BSA for another hour. After extensive washes in PBS-Tween 0.05%, the amount of bodipy–ANA-12 bound is quantified by fluorescence at 520 ± 10 nm. Detectability range for extrapolation analysis is assessed by coating ELISA plates with bodipy–ANA-12 and reading fluorescence at 520 ± 10 nm.

细胞实验

Modulation of neurite outgrowth by molecules is assessed in nnr5 PC12–TrkB, –TrkA, and –TrkC cells after addition of BDNF (1 nM), NGF (2 nM), and NT-3 (10 nM), respectively. The number of cells bearing neurites longer than 2 cells in diameter in each counting field is microscopically determined (2 fields per well, 3 wells per condition). Counting is performed blind each 24 hours for 3 days. (Only for Reference)

Cas No.

219766-25-3

分子式

C22H21N3O3S

分子量

407.49

别名

ANA 12;ANA12

储存和溶解度

Ethanol:<1 mgml
H2O:<1 mgml
DMSO:35 mg/mL (85.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years