SUN11602

产品编号: T3714 别名:

SUN 11602

SUN 11602 是新型的碱性苯胺化合物，具有成纤维细胞生长因子特性。

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CAS：704869-38-5

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

SUN11602, an aniline compound, mimics the neuroprotective mechanisms of basic fibroblast growth factor. It mimics the neuroprotective effects of bFGF and prevents glutamate-induced neuronal death. It also increases levels of CALB1 gene expression in cerebrocortical neurons and triggers phosphorylation of FGFR and ERK1/2.

体外活性

Physiological actions of SUN11602 mimic several phenomena of the neuroprotection that is induced by bFGF. SUN11602 plays a pivotal role in allowing primary cultured neurons to survive in adverse environments of glutamate toxicity and activating intracellular key molecules that are involved in the neuroprotective mechanisms. These actions are quite similar to those of bFGF. Such neuroprotective mechanisms are specific and distinctive to SUN11602 and bFGF and differs clearly from those of the other growth factors that are investigated. But unlike bFGF, SUN11602 can either directly or indirectly trigger the phosphorylation of the cytosolic domain of the FGFR without binding to the extracellular domain of the FGFR-1[1]. SUN11602 demonstrates no cell proliferative activity of somatic cells, unlike bFGF. SUN11602 significantly affects neuronal survival in adverse conditions through a FGFR1-mitogen-activated protein kinase/extracellular signal-regulated kinase-1/2 kinase (FGFR-1–MEK/ERK) signaling pathway[2].

体内活性

In WT mice, SUN11602 and bFGF increase the levels of newly synthesized Calb in cerebrocortical neurons and suppress the glutamate-induced rise in intracellular Ca2+. This Ca2+-capturing ability of Calb allows the neurons to survive severe toxic conditions of glutamate. In contrast, Calb levels remain unchanged in Calb-/- mice after exposure to SUN11602 or bFGF, and due to a loss of function of the gene, these neurons are no longer resistant to toxic conditions of glutamate[1]. Neuroprotective activities of SUN11602 and FGF-2 are due to exogenously induced hyperexpression of CalB in hippocampal neurons. The pharmacokinetic properties of SUN11602 appear to hold promise in terms of bioavailability (>65%) after oral administration in rodents (rats and mice) and dogs (beagles)[2].

细胞实验

Actinomycin D or cycloheximide is first added to the cultures, and, 2 h later, SUN11602 or bFGF is added. After a 24 h incubation, neurons in the cultures are exposed to 150 μM glutamate for another 24 h, and cell viability is determined by a (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H tetrazolium bromide (MTT) assay.(Only for Reference)

Cas No.

704869-38-5

分子式

C26H37N5O2

分子量

451.615

别名

SUN 11602;SUN11602

参考文献

[1]Murayama N, et al. Brain Res. 2015, 1594:71-81.[2]Murayama N, et al. ACS Chem Neurosci. 2013, 4(2):266-76.

储存和溶解度

Ethanol:9 mg/mL (20 mM)
DMSO:22.6 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 SUN11602 704869-38-5

对于各种应用，安全且有效的用药剂量是很有必要的了解更多

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第一步：请输入动物实验的基本信息

剂量 mg/kg

每只动物体重 g

给药体积 ul

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO +

% +

% Tween 80 +

% ddH₂O

% DMSO +

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计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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技术支持

在抑制剂处理说明中可以找到您可能遇到的问题的答案。主题包括如何准备储备溶液，如何存储产品以及基于细胞的测定和动物实验需要特别注意的问题。

Keywords

inhibit SUN 11602 Fibroblast growth factor receptor SUN11602 FGFR Inhibitor SUN-11602 704869-38-5

SUN11602 相关推荐

相关化合物库推荐该产品包含在如下化合物库中：

注册成功

SUN11602

SUN 11602

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