1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Betahistine dihydrochloride

Betahistine dihydrochloride  (Synonyms: 盐酸倍他司汀)

目录号: HY-B0524A 纯度: 99.74%
COA 产品使用指南

Betahistine dihydrochloride 是一种口服有效的组胺 H1 受体 (histamine H1 receptor) 激动剂和 H3 受体 (H1 receptor) 的拮抗剂。Betahistine dihydrochloride 用于类风湿性关节炎 (RA) 的研究。

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Betahistine dihydrochloride Chemical Structure

Betahistine dihydrochloride Chemical Structure

CAS No. : 5579-84-0

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10 mM * 1 mL in DMSO ¥550
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1 g ¥200
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5 g ¥450
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Other Forms of Betahistine dihydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].

IC50 & Target[1]

H3 Receptor

 

体外研究
(In Vitro)

Betahistine dihydrochloride (0-10 μM) inhibits [125I]iodoproxyfan binding to membranes of CHO (rH3(445)R) and CHO (hH3(445)R) cells with IC50 values of 1.9 μM and 3.3 μM, respectively. Lead to Ki values of 1.4 μM and 2.5 μM, respectively[2].
Betahistine dihydrochloride (0-10 μM) has a regulating function on cAMP formation in CHO (rH3(445)R), CHO (rH3(413)R), and CHO (hH3(445)R) cells. At low concentrations, betahistine behaves an apparent inverse agonist, and progressively enhances cAMP formation with EC50 values of 0.1 nM, 0.05 nM and 0.3 nM, respectively. In contrast, at concentrations higher than 10 nM, betahistine inhibits cAMP formation with an EC50 value of 0.1 μM in CHO (rH3(445)R) and full agonist activity[2].

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

体内研究
(In Vivo)

Betahistine dihydrochloride (intraperitoneal or oral administration; 0.1-30 mg/kg; single dose) with acute administration has increased tele-methylhistamine (t-MeHA) levels with an ED50 of 0.4 mg/kg, indicating the inverse agonism. Besides, after acute oral administration, it increases t-MeHA levels with an ED50 of 2 mg/kg in male Swissmice[2].
Betahistine dihydrochloride (oral adminstration; 1 and 5 mg/kg; daily for 3 weeks) attenuates the severity of arthritis and reduces the levels of pro-inflammatory cytokines in the paw tissues of CIA mice[3].

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

Animal Model: Collagen-induced arthritis (CIA) DBA/1 male mouse model[3]
Dosage: 1 mg/kg; 5mg/kg
Administration: Oral adminstration; day 21 to day 42 after a 21-day CIA induction
Result: Ameliorated mouse CIA by decreasing joint destruction.
Clinical Trial
分子量

209.12

Formula

C8H14Cl2N2

CAS 号
性状

固体

颜色

White to off-white

中文名称

盐酸倍他司汀;倍他司丁二盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

H2O 中的溶解度 : ≥ 50 mg/mL (239.10 mM)

DMSO 中的溶解度 : 33.33 mg/mL (159.38 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)

DMF 中的溶解度 : 5 mg/mL (23.91 mM; 超声助溶)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.7819 mL 23.9097 mL 47.8194 mL
5 mM 0.9564 mL 4.7819 mL 9.5639 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 (protect from light, stored under nitrogen)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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

In Vivo:

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 150 mg/mL (717.29 mM); 澄清溶液; 超声助溶

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
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料
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 (protect from light, stored under nitrogen)。-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
DMF / DMSO / H2O 1 mM 4.7819 mL 23.9097 mL 47.8194 mL 119.5486 mL
5 mM 0.9564 mL 4.7819 mL 9.5639 mL 23.9097 mL
10 mM 0.4782 mL 2.3910 mL 4.7819 mL 11.9549 mL
15 mM 0.3188 mL 1.5940 mL 3.1880 mL 7.9699 mL
20 mM 0.2391 mL 1.1955 mL 2.3910 mL 5.9774 mL
DMSO / H2O 25 mM 0.1913 mL 0.9564 mL 1.9128 mL 4.7819 mL
30 mM 0.1594 mL 0.7970 mL 1.5940 mL 3.9850 mL
40 mM 0.1195 mL 0.5977 mL 1.1955 mL 2.9887 mL
50 mM 0.0956 mL 0.4782 mL 0.9564 mL 2.3910 mL
60 mM 0.0797 mL 0.3985 mL 0.7970 mL 1.9925 mL
80 mM 0.0598 mL 0.2989 mL 0.5977 mL 1.4944 mL
100 mM 0.0478 mL 0.2391 mL 0.4782 mL 1.1955 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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:
Betahistine dihydrochloride
目录号:
HY-B0524A
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