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SML0209

ANA-12

Name: ANA-12
Brand: SIGMA

≥98% (HPLC), TrkB antagonist, powder

别名:

N- [2-[[（六氢-2-氧代-1H-氮杂卓-3-基）氨基]羰基]苯基]-苯并[b]噻吩-2-甲酰胺

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关于此项目

经验公式（希尔记法）:

C₂₂H₂₁N₃O₃S

化学文摘社编号:

219766-25-3

分子量:

407.49

UNSPSC Code:

51111800

PubChem Substance ID:

329825231

NACRES:

NA.77

MDL number:

MFCD00117444

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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属性

产品名称

ANA-12, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: ≥5 mg/mL at 60 °C

storage temp.

2-8°C

SMILES string

O=C1NCCCCC1NC(=O)c2ccccc2NC(=O)c3cc4ccccc4s3

InChI

1S/C22H21N3O3S/c26-20(25-17-10-5-6-12-23-21(17)27)15-8-2-3-9-16(15)24-22(28)19-13-14-7-1-4-11-18(14)29-19/h1-4,7-9,11,13,17H,5-6,10,12H2,(H,23,27)(H,24,28)(H,25,26)

InChI key

TUSCYCAIGRVBMD-UHFFFAOYSA-N

说明

Application

ANA-12用于抑制原代小鼠皮层神经元和原代大鼠海马培养物中的TrkB。

Biochem/physiol Actions

TrkB拮抗剂在小鼠中具有有效的抗焦虑样和抗抑郁样活性

神经营养素脑源性神经营养因子（BDNF）及其受体原肌球蛋白相关激酶B（TrkB）已成为几种情绪障碍（包括焦虑症和抑郁症）的病理生理学的关键介体。ANA-12是一种TrkB配体，可有效阻止BDNF激活受体。它选择性地与TrkB结合并抑制TrkB下游的过程，而不会改变TrkA和TrkC的功能。在成年小鼠中，ANA-12模型可降低大脑中TrkB的活性，而不会影响神经元的存活。给予 ANA-12 的小鼠在预测人类抗焦虑和抗抑郁特性的各种试验中显示焦虑和抑郁相关行为减少。ANA-12 可能是研究 BDNF/TrkB 信号的一种有价值的工具，并可能构成开发下一代治疗心境障碍药物的先导化合物。还有 N-T19，其效价较低。

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pictograms

GHS07

signalword

Warning

hcodes

H302

pcodes

P264 - P270 - P301 + P312 - P501

Hazard Classifications

Acute Tox. 4 Oral

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

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Lot/Batch Number

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Role of AMPA receptor stimulation and TrkB signaling in the antidepressant-like effect of ketamine co-administered with a group II mGlu receptor antagonist, LY341495, in the forced swim test in rats.

Agnieszka Pałucha-Poniewiera et al.

Behavioural pharmacology, 30(6), 471-477 (2019-02-07)

Ketamine has been shown to induce a rapid antidepressant effect on patients with depression. In many animal models, both rapid and sustained antidepressant activities were also found in response to an antagonist of group II metabotropic glutamate receptors, LY341495, and

Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice.

Maxime Cazorla et al.

The Journal of clinical investigation, 121(5), 1846-1857 (2011-04-21)

The neurotrophin brain-derived neurotrophic factor (BDNF) and its receptor tropomyosin-related kinase B (TrkB) have emerged as key mediators in the pathophysiology of several mood disorders, including anxiety and depression. However, therapeutic compounds that interact with TrkB receptors have been difficult

Tissue-type plasminogen activator protects the postsynaptic density in the ischemic brain.

Valerie Jeanneret et al.

Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 38(11), 1896-1910 (2018-03-17)

Cerebral ischemia causes the presynaptic release of tissue-type plasminogen activator (tPA). The postsynaptic density (PSD) is a postsynaptic structure that provides a matrix where signaling transduction of excitatory synapses takes place. The postsynaptic density protein-95 (PSD-95) is the most abundant

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全球贸易项目编号

货号	GTIN
SML0209-25MG	04061833222126
SML0209-5MG	04061833222133