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Betahistine dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Betahistine dihydrochloride图片
CAS NO:5579-84-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
200mg电议
500mg电议

产品名称
盐酸倍他司汀
产品介绍
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。
生物活性

Betahistine dihydrochloride is an orally activehistamine H1 receptoragonist and aH3 receptorantagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].

IC50& Target[1]

H3Receptor

 

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 withIC50values of 1.9 μM and 3.3 μM, respectively. Lead to Kivalues 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 EC50values 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 EC50value of 0.1 μM in CHO (rH3(445)R) and full agonist activity[2].

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 ED50of 0.4 mg/kg, indicating the inverse agonism. Besides, after acute oral administration, it increases t-MeHA levels with an ED50of 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].

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

性状

Solid

Formula

C8H14Cl2N2

CAS 号

5579-84-0

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 : ≥ 50 mg/mL(239.10 mM)

DMSO : 33.33 mg/mL(159.38 mM;Need ultrasonic)

DMF : 5 mg/mL(23.91 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.7819 mL23.9097 mL47.8194 mL
5 mM0.9564 mL4.7819 mL9.5639 mL
10 mM0.4782 mL2.3910 mL4.7819 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℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 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

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 150 mg/mL (717.29 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。