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Harmine
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。
Harmine图片
CAS NO:442-51-3

去氢骆驼蓬碱
Telepathine
Harmine 是一种具有抗癌和抗炎活性的天然双特异性酪氨酸磷酸化调节激酶 (DYRK) 抑制剂。Harmine 对5-HT2A血清素受体具有高亲和力,Ki值为 397 nM。
生物活性

Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of5-HT2Aserotonin receptor, with anKiof 397 nM[1].

IC50& Target[1][2]

DYRK1

 

DYRK1A

 

5-HT2AReceptor

397 nM (Ki)

体外研究
(In Vitro)

Harmine inhibits tau phosphorylation by DYRK1A by selected DANDYs, with an IC50of 190 nM[2].Harmine negatively regulates homologous recombination (HR) by interfering Rad51 recruitment, resulting in severe cytotoxicity in hepatoma cells. Furthermore, NHEJ inhibitor Nu7441 markedly sensitizes Hep3B cells to the anti-proliferative effects of Harmine[3].

体内研究
(In Vivo)

It is shown that brain water content is significantly increased in the TBI group. Treatment with Harmine significantly reduces the tissue water content at 1, 3 and 5 days, compared with the TBI group. Harmine treatment significantly reduces the escape latency at 3 and 5 days, compared with the TBI group. Post-TBI administration of Harmine significantly improves the motor function recovery of the rats at 1, 3 and 5 days following TBI, compared with the TBI group without Harmine treatment. The neuronal survival rate in the Harmine-treated group is significantly increased, compared with the TBI group. Administration of Harmine results in marked elevation in the expression of GLT-1, compared with the TBI group. The administration of Harmine significantly reduces the expression of caspase 3, compared with the TBI group[4].

Clinical Trial
分子量

212.25

性状

Solid

Formula

C13H12N2O

CAS 号

442-51-3

中文名称

去氢骆驼蓬碱;肉叶芸香碱;哈尔明碱

结构分类
  • Alkaloids
  • Indole Alkaloids
来源
  • Plants
  • Zygophyllaceae
  • Peganum harmalaLinn.
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 30 mg/mL(141.34 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.7114 mL23.5571 mL47.1143 mL
5 mM0.9423 mL4.7114 mL9.4229 mL
10 mM0.4711 mL2.3557 mL4.7114 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (11.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.78 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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 ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (11.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.78 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。
 
 
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