首页 GPCR/G Protein Histamine Receptor H3R-IN-1 Hydrochloride
H3R-IN-1 Hydrochloride
编号 T11531    
CAS T11531     分子式 C19H24ClN3O3     分子量 377.87
靶点: Histamine receptor 3;
H3R-IN-1 Hydrochloride is an inverse agonist of histamine receptor 3 (H3R).
选择批次  
纯度 98.00%
规格 库存 单价 数量
5 mg 待询 3010.00
10 mg 待询 4710.00
25 mg 待询 9385.00
50 mg 待询 14910.00
100 mg 待询 23410.00
200 mg 待询 待询
500 mg 待询 待询
1 mL * 10 mM (in DMSO) 待询 3310.00
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生物活性

产品描述

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

靶点活性

Histamine receptor 3,

体外活性

H3R-IN-1 increases the Forskolin-stimulated cAMP level in the primary oligodendrocyte precursor cells in a dose-dependent manner.Treatment with H3R-IN-1, which is a H3R inverse agonist, promotes oligodendrocyte precursor cell (OPC) differentiation in a dose-dependent manner, at EC50=25 nM. Western blot reveals 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 suggests that treatment with H3R-IN-1 drives more OPCs to differentiate.

体内活性

The ability of H3R-IN-1 to enhance in vivo remyelination is determined with 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.

化学信息

分子量

377.87

分子式

C19H24ClN3O3

CAS

T11531

溶解度

DMSO: 25 mg/mL (66.16 mM), Need warming

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.646 ml 13.232 ml 26.464 ml
5 mM 0.529 ml 2.646 ml 5.293 ml
10 mM 0.265 ml 1.323 ml 2.646 ml
50 mM 0.053 ml 0.265 ml 0.529 ml
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