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H3R-IN-1 Hydrochloride
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。
H3R-IN-1 Hydrochloride图片
包装与价格:
包装价格(元)
50 mg电议
100 mg电议

产品介绍
H3R-IN-1 Hydrochloride 是一种有效的组胺H3受体 (H3R) 的反向激动剂。

产品描述

H3R-IN-1 Hydrochloride is an inverse agonist of histamine receptor 3( H3R ) .

体外活性

Treatment with H3R-IN-1, which is a H3R inverse agonist, promotes oligodendrocyte precursor cell (OPC) differentiation in a dose-dependent manner, at EC 50 =25 nM. Western blot shows a significant increase in expression levels of two markers of mature oligodendrocytes, myelin-associated glycoprotein (MAG) and myeline basic protein (MBP) in differentiating oligodendrocytes after treatment with H3R-IN-1, which reveals that treatment with H3R-IN-1 drives more OPCs to differentiate. H3R-IN-1 increases the Forskolin-stimulated cAMP level in the primary oligodendrocyte precursor cells in a dose-dependent manner [1].

体内活性

The ability of H3R-IN-1 to enhance remyelination in vivo is determined using the Cuprizone/Rapamycin-induced demyelination model. Mice are treated with Cuprizone diet combined with intraperitoneal injections of Rapamycin for 5 weeks followed by 9 days of compound administration. Cuprizone diet plus intraperitoneal injections of Rapamycin induced severe demyelination in both corpus callosum and cortex and treatment with H3R-IN-1 (30 mg/kg, 9 days) significantly increases density of myelin specific Black-gold II staining in the lesion of corpus callosum and cortex in forebrain, compared to vehicle control group [1].

Cas No.

T11531

分子式

C19H24ClN3O3

分子量

377.87

别名

H3R-IN-1 Hydrochloride

储存和溶解度

DMSO:25 mg/mL (66.16 mM),Need warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years