基本信息
产品编号: |
B10220 |
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产品名称: |
Betahistine |
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CAS: |
5638-76-6 |
储存条件 |
粉末 |
室温 |
四年 |
分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
136.20 |
-20℃ |
1个月 |
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化学名: |
N-methyl-2-(pyridin-2-yl)ethan-1-amine |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
7.3427mL |
36.7134mL |
73.4268mL |
5mM |
1.4685mL |
7.3427mL |
14.6854mL |
10mM |
0.7343mL |
3.6713mL |
7.3427mL |
生物活性
产品描述 |
一种组胺类似物和H1受体激动剂,作为血管扩张剂。 |
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靶点 |
H1 Receptor |
H3 receptor |
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体外研究 |
Betahistine (0-10μM) inhibits [125I]iodoproxyfan binding to membranes of CHO (rH3(445)R) and CHO (hH3(445)R) cells with IC50 values of 1.9μM and 3.3μM,respectively.Lead to Ki values of 1.4μM and 2.5μM,respectively.Betahistine (0-10μM) 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 0.1nM,0.05nM and 0.3nM,respectively.In contrast,at concentrations higher than 10nM,betahistine inhibits cAMP formation with an EC50 value of 0.1μM in CHO (rH3(445)R) and full agonist activity. |
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体内研究 |
Betahistine (intraperitoneal or oral administration;0.1-30mg/kg;single dose) with acute administration has increased telemethylhistamine (t-MeHA) levels with an ED50 of 0.4mg/kg,indicating the inverse agonism.Besides,after acute oral administration,it increases t-MeHA levels with an ED50 of 2mg/kg in male Swissmice.Betahistine (oral adminstration;1 and 5mg/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. |
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Animal Model: |
Collagen-induced arthritis (CIA) DBA/1 male mouse model |
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Dosage: |
1mg/kg;5mg/kg |
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Administration: |
Oral adminstration;day 21 to day 42 after a 21-day CIA induction |
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Result: |
Ameliorated mouse CIA by decreasing joint destruction. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )