1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. H3R antagonist 1

H3R antagonist 1 是组胺受体 3 (H3R) 的反向激动剂。H3R antagonist 1 可增加分化少突胶质细胞中髓鞘相关糖蛋白 (MAG) 和髓鞘碱性蛋白 (MBP) 的表达水平。H3R antagonist 1 可用于多发性硬化症的研究。

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H3R antagonist 1 Chemical Structure

H3R antagonist 1 Chemical Structure

CAS No. : 1448422-61-4

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Other Forms of H3R antagonist 1:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

H3R antagonist 1 is a histamine receptor 3 (H3R) inverse agonist. H3R antagonist 1 increases the expression levels of myelin-associated glycoprotein (MAG) and myeline basic protein (MBP) in differentiating oligodendrocytes. H3R antagonist 1 can be used for the study of multiple sclerosis[1].

IC50 & Target

Histamine receptor 3[1]

体外研究
(In Vitro)

H3R antagonist 1 (example 2) 以剂量依赖性方式促进少突胶质细胞前体细胞 (OPC) 分化,EC50 = 25 nM。Western blot 检测显示,经 H3R antagonist 1 处理后,分化中的少突胶质细胞中两种成熟少突胶质细胞标志物——髓鞘相关糖蛋白 (MAG) 和髓鞘碱性蛋白 (MBP) 的表达水平显著增加,这表明 H3R antagonist 1 处理可促进更多少突胶质细胞前体细胞分化。 H3R antagonist 1 以剂量依赖性方式增加原代少突胶质细胞前体细胞中 Forskolin (HY-15371) 刺激的 cAMP 水平[1]

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

体内研究
(In Vivo)

采用 Cuprizone (HY-W115718)/Rapamycin (HY-10219) 诱导的脱髓鞘模型,测定 H3R antagonist 1 (example 2) 增强体内髓鞘再生的能力。小鼠接受 Cuprizone 饮食联合腹膜内注射 Rapamycin 治疗 5 周,随后给予化合物 9 天。与载体对照组相比,Cuprizone 饮食联合腹膜内注射 Rapamycin 可诱导胼胝体和皮质发生严重脱髓鞘,而用 H3R antagonist 1 (example 2) (30 mg/kg,9 天) 治疗可显著增加前脑胼胝体和皮质病变中髓鞘特异性黑金 II 染色的密度[1]

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

分子量

341.40

Formula

C19H23N3O3

CAS 号
性状

固体

颜色

White to off-white

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)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (292.91 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9291 mL 14.6456 mL 29.2912 mL
5 mM 0.5858 mL 2.9291 mL 5.8582 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Animal Administration
[1]

Mice[1]
The C57BL/6 mice at age of 8 weeks are fed with powder mouse food mixed freshly with 0.2% Cuprizone (w/w) and receive daily intraperitoneal injection of Rapamycin (10 mg/kg body weight) for 5 weeks to induce demyelination, then animals are allowed to recover (removal of Cuprizone from the diet and Rapamycin injection) and administrated with H3R-IN-1, at 30 mg/kg body weight orally, b.i.d. for an additional 9 days prior to sacrifice. The brain samples are collected for pathologic analysis[1].

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

参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9291 mL 14.6456 mL 29.2912 mL 73.2279 mL
5 mM 0.5858 mL 2.9291 mL 5.8582 mL 14.6456 mL
10 mM 0.2929 mL 1.4646 mL 2.9291 mL 7.3228 mL
15 mM 0.1953 mL 0.9764 mL 1.9527 mL 4.8819 mL
20 mM 0.1465 mL 0.7323 mL 1.4646 mL 3.6614 mL
25 mM 0.1172 mL 0.5858 mL 1.1716 mL 2.9291 mL
30 mM 0.0976 mL 0.4882 mL 0.9764 mL 2.4409 mL
40 mM 0.0732 mL 0.3661 mL 0.7323 mL 1.8307 mL
50 mM 0.0586 mL 0.2929 mL 0.5858 mL 1.4646 mL
60 mM 0.0488 mL 0.2441 mL 0.4882 mL 1.2205 mL
80 mM 0.0366 mL 0.1831 mL 0.3661 mL 0.9153 mL
100 mM 0.0293 mL 0.1465 mL 0.2929 mL 0.7323 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
H3R antagonist 1
目录号:
HY-112219
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