ANA 12
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ANA 12是TrkB的有效选择性拮抗剂,在高亲和力位点和低亲和力位点的IC50值分别为45.6 nM和41.1 μM[1].
原肌球蛋白相关激酶B(TrkB)是脑源性神经营养因子(BDNF)和神经营养蛋白4/5(NT-4/5)的受体,激活3个主要的信号通路,包括磷脂酶C-γ\PI3K和MAPK.BDNF/TrkB信号在药物成瘾\抑郁和焦虑中发挥重要作用[1].
ANA 12是TrkB的有效选择性拮抗剂.ANA-12以剂量依赖性方式结合到TrkB的胞外低亲和性位点,Kd值为12 μM.ANA-12结合于高亲和力位点的Kd值为10 nM.此外,ANA-12以非竞争性机制与TrkB结合.在表达TrkB的细胞中,10 nM 的ANA-12有效抑制BDNF诱导的轴突生长,并完全消除10-100 μM BDNF的效应[1].
在小鼠脑内,0.5 mg/kg 的ANA-12处理4个小时后,抑制25%的内源性TrkB活性.此外,ANA-12具有抗抑郁和抗焦虑活性[1].
参考文献:
[1]. Cazorla M, Prémont J, Mann A, et al. Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J Clin Invest, 2011, 121(5): 1846-1857.
- 1. Jing Zhao, Peifeng Li, et al. "7, 8-Dihydroxyflavone suppresses proliferation and induces apoptosis of human osteosarcoma cells." Acta Biochim Biophys Sin (Shanghai). 2021 Jul 5;53(7):903-911. PMID: 34019097
- 2. Wang Z, Wang SP, et al. "Brain-derived neurotrophic factor mimetic, 7,8-dihydroxyflavone, protects against myocardial ischemia by rebalancing optic atrophy 1 processing." Free Radic Biol Med. 2019 Sep 28;145:187-197. PMID: 31574344
- 3. Zhao J, Du J, et al. "Activation of cardiac TrkB receptor by its small molecular agonist 7,8-dihydroxyflavone inhibits doxorubicin-induced cardiotoxicity via enhancing mitochondrial oxidative phosphorylation." Free Radic Biol Med. 2019 Jan;130:557-567. PMID: 30472367
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 407.49 |
Cas No. | 219766-25-3 |
Formula | C22H21N3O3S |
Solubility | insoluble in H2O; insoluble in EtOH; ≥10.175 mg/mL in DMSO with gentle warming |
Chemical Name | N-(2-((2-oxoazepan-3-yl)carbamoyl)phenyl)benzo[b]thiophene-2-carboxamide |
SDF | Download SDF |
Canonical SMILES | O=C(NC1CCCCNC1=O)C2=CC=CC=C2NC(C3=CC4=CC=CC=C4S3)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
酶学实验[1]: | |
激酶检测 |
用各种浓度的TrkBECD-Fc,20mg/ml BSA或1mg/ml IgG-Fc在碳酸盐缓冲液(pH9.6)中包被Maxisorp ELISA 96孔平板,4℃过夜。在室温下用0.5%BSA的PBS将板饱和2小时,并用0.05%的PBS-Tween洗涤。然后在室温下,将Bodipy-ANA-12在0.5%PBS-BSA中孵育1小时,然后加入BDNF再孵育1小时。在PBS-Tween 0.05%充分洗涤后,在520±10nm的荧光下检测bodipy-ANA-12的量。 |
细胞实验[1]: | |
细胞系 |
PC12-TrkB细胞系 |
溶解方法 |
在DMSO中的溶解度> 10 mM。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
0-100 μM,3天 |
应用 |
在TrkB表达细胞中,ANA-12在低至10nM的浓度下阻止脑源性神经营养因子诱导的神经突生长。在高达10-100μM的浓度下,ANA-12可完全消除脑源性神经营养因子的作用,观察不到单个神经突或分支。 |
动物实验[1]: | |
动物模型 |
小鼠 |
剂量 |
0.5 mg/kg |
应用 |
给予ANA-12的小鼠在预测人类抗焦虑和抗抑郁药物性质的各种测试中表现出减少的焦虑和抑郁相关行为。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Cazorla M, Prémont J, Mann A, et al. Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J Clin Invest, 2011, 121(5): 1846-1857. |
质量控制和MSDS
- 批次: