H3R antagonist 1 hydrochloride - 10mM in DMSO, high purity , CAS No.2319790-07-1(DMSO)

Item Number

H654707

• Specifications & Purity: 10mM in DMSO
• Storage Temp: Desiccated,Store at -80°C
• Shipped In: Ice chest + Ice pads

Product Description

H3R antagonist 1 hydrochloride is a histamine receptor 3 ( H3R ) inverse agonist extracted from patent WO2013107336A1, compound example 2.

In Vitro

Treatment with H3R antagonist 1 hydrochloride, which is a H3R inverse agonist, promotes oligodendrocyte precursor cell (OPC) differentiation in a dose-dependent manner, at EC 50 =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 antagonist 1 hydrochloride, which suggests that treatment with H3R antagonist 1 hydrochloride drives more OPCs to differentiate. H3R antagonist 1 hydrochloride increases the Forskolin-stimulated cAMP level in the primary oligodendrocyte precursor cells in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The ability of H3R antagonist 1 hydrochloride-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 antagonist 1 hydrochloride (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:H 3 receptor