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CFM-2
AMPA拮抗剂,CFM-2是AMPAR选择非竞争性抑制剂。
目录号: PC12161 纯度: ≥98%
CAS No. :178616-26-7
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中文名称
CFM-2
中文别名
1-(4-氨基苯基)-3,5-二氢-7,8-二甲氧基-4H-2,3-苯并二氮杂-4-酮;1-(4-氨基苯基)-3,5-二氢-7,8-二甲氧基-4H-2,3-苯并二氮杂卓-4-酮;1-(4'-AMINOPHENYL)-3,5-DIHYDRO-7,8-DIMETHOXY-4H-2,3-BENZODIAZEPIN-4-ONE
英文名称
CFM-2
英文别名
4H-2,3-Benzodiazepin-4-one,1-(4-aminophenyl)-3,5-dihydro-7,8-dimethoxy-;1-(4-aminophenyl)-7,8-dimethoxy-3,5-dihydro-2,3-benzodiazepin-4-one;CFM-2;1-(4’-AMINOPHENYL)-3,5-DIHYDRO-7,8-DIMETHOXY-4H-2,3-BENZODIAZEPIN-4-ONE;1-(4'-AMinophenyl)-3,5-dihydro-7,8-diMethoxy-4H-2,3-benzodiazepin-4-one;Eeyarestatin I;Tocris-1082;CFM 2
Cas No.
178616-26-7
分子式
C17H17N3O3
分子量
311.34
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

CFM-2 is a potent and selective non-competitive AMPAR antagonist. CFM-2 possesses anticonvulsant activity in various models of seizures.

性状

Solid

IC50 & Target[1][2]

AMPA Receptor

 

体外研究(In Vitro)

CFM-2 inhibits the extracellular signal regulated kinase (ERK1/2) pathway, CFM-2 reduced phosphorylation of cAMP-responsive element binding protein (CREB), suppressed expression of cyclin D1, upregulated the cell cycle regulators and tumor suppressor proteins p21 and p53 and decreased number of lung adenocarcinoma cells in G2 and S phases of the cell cycle.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Pretreatment with CFM-2 delays the progression of seizure rank during repeated administration of pentylentetrazole. At the end of the period of repeated pentylentetrazole treatment (6 weeks) the mean seizure score was 0 in vehicle treated controls, 4.3 in animals treated with vehicle + pentylentetrazole, 2.2 in rats treated chronically with CFM-2 (20 μmol/kg; i.p.) + pentylentetrazole and 1.0 in rats treated repeatedly with CFM-2 (50 μmol/kg; i.p.) + pentylenetetrazole. CFM-2 is also able to antagonize the long-term increase in sensitivity of the convulsant effects of GABA function inhibitors in pentylentetrazole-kindled animals.
Intrathecal application of two selective non-competitive AMPAR antagonists, CFM-2 (25 and 50 μg) and GYKI 52466 (50μg), significantly attenuated mechanical and thermal hypersensitivities on the ipsilateral hind paw at 2 and 24 h post-CFA injection. Neither CFM-2 nor GYKI 52466 affects the contralateral basal responses to thermal and mechanical stimuli.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : ≥ 50 mg/mL (160.60 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2119 mL 16.0596 mL 32.1192 mL
5 mM 0.6424 mL 3.2119 mL 6.4238 mL
10 mM 0.3212 mL 1.6060 mL 3.2119 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (8.83 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (8.83 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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