H3R antagonist 1 hydrochloride,95.52%

产品编号:Bellancom-112219A| CAS NO:2319790-07-1| 分子式:C19H24ClN3O3| 分子量:377.87

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-112219A
3500.00 杭州 北京(现货)
Bellancom-112219A
5500.00 杭州 北京(现货)
Bellancom-112219A
11000.00 杭州 北京(现货)
Bellancom-112219A
17500.00 杭州 北京(现货)
Bellancom-112219A
27500.00 杭州 北京(现货)

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H3R antagonist 1 hydrochloride

产品介绍 H3R antagonist 1 hydrochloride 是一种有效的组胺受体 3 (H3R) 反向激动剂,详细信息请参考专利文献 WO2013107336A1 中的化合物 2。
生物活性

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

体外研究

Treatment with H3R antagonist 1 hydrochloride, 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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状Solid
溶解性数据
In Vitro: 

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

H2O : 25 mg/mL (66.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6464 mL 13.2321 mL 26.4641 mL
5 mM 0.5293 mL 2.6464 mL 5.2928 mL
10 mM 0.2646 mL 1.3232 mL 2.6464 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

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