哈尔碱盐酸盐(水合)

中文名称:

哈尔碱盐酸盐(水合)

中文同义词:

哈尔碱盐酸盐(水合);骆驼蓬碱盐酸盐;水合哈尔碱盐酸盐;盐酸-7-甲氧基-1-甲基-9H-吡啶并(3,4-B)吲哚;盐酸哈尔明;罗勒生物碱;哈尔明盐酸盐;盐酸去氢骆驼蓬碱

英文名称:

HARMINE HYDROCHLORIDE

英文同义词:

HarMine.HC;7-METHOXY-1-METHYL-9H-PYRIDO[3,4-B]INDOLE HCL;(3,4-b)indole,7-Methoxy-1-Methyl-9h-pyrido(Monohydrochloride;BANISTERINE HYDROCHLORIDE;BANISTERIN HCL;HARMINE HCL;HARMINE HYDROCHLORIDE;4-b)indole,7-methoxy-1-methyl-9h-pyrido(monohydrochloride

CAS号:

343-27-1

分子式:

C13H13ClN2O

分子量:

248.71

EINECS号:

206-443-8

相关类别:

中草药成分;中药对照品;标准品;标准品-对照品;小分子抑制剂，天然产物;合成;中药标准品;植物提取物;chemical reagent;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;对照品;植提标准品;医药原料;标准品-中药标准品;标准品 -中药标准品;植物成分单体;标准品，对照品;化工原料;单体化合物;Alkaloids;Biochemistry;Indole Alkaloids;standardized herbal extract;Inhibitors

Mol文件:

343-27-1.mol

熔点 

265-270°C

储存条件 

2-8°C

形态

powder

颜色

off-white to pale green

Merck 

14,4616

CAS 数据库

343-27-1(CAS DataBase Reference)

EPA化学物质信息

Harmine hydrochloride (343-27-1)

生物活性

Harmine (Telepathine)是属于β-咔啉家族化合物的一种荧光harmala生物碱，是一种高细胞渗透性的 DYRK1A 的激酶口袋结合ATP的竞争性抑制剂，与DYRK2结合IC50值高约60倍。Harmine 还可以抑制 monoamine oxidases (MAOs) 和 cdc-like kinases (CLKs)。Harmine 抑制 5-HT2A serotonin receptor 的Ki值为397 nM。

靶点

Target Value DYRK1A (Cell-free assay) 33 nM MNB (Cell-free assay) 149 nM DYRK1B (Cell-free assay) 166 nM DYRK2 (Cell-free assay) 1.9 μM

Target

Value

DYRK1A (Cell-free assay)

33 nM

MNB (Cell-free assay)

149 nM

DYRK1B (Cell-free assay)

166 nM

DYRK2 (Cell-free assay)

1.9 μM

体外研究

Harmine inhibits tau phosphorylation by DYRK1A by selected DANDYs, with an IC 50 of 190 nM. 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.

体内研究

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.

化学性质 

黄色结晶粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于骆驼蓬。

用途 

盐酸去氢骆驼蓬碱具有抗肿瘤的作用。

用途 

用于含量测定/鉴定/药理实验等。 药理药效:杀菌、止痒，抗银屑病作用，抗肿瘤作用。

类别

有毒物质

毒性分级

高毒

急性毒性

静脉- 小鼠 LD50: 38 毫克/公斤

可燃性危险特性

可燃, 燃烧时分解有毒氯化物, 氮氧化物气体

储运特性

库房低温, 通风, 干燥; 与食品原料分开存放

灭火剂

水, 二氧化碳, 泡沫, 砂土

危险品标志 

Xn

危险类别码 

20/21/22-40

安全说明 

22-36

危险品运输编号 

1544

WGK Germany 

3

RTECS号

MG9450000

HazardClass 

6.1(b)

PackingGroup 

III

海关编码 

29339900