马来酸氯苯那敏 T1553

Product Introduction
Bioactivity


英文名: Chlorpheniramine maleate

描述: Chlorpheniramine maleate (NCI-C55265) 是一种组胺 H1 拮抗剂，IC50为12 nM，用于过敏反应、花粉热、鼻炎、荨麻疹和哮喘。

细胞实验: Cells are exposed to various concentrations of Chlorpheniramine for 48 hours. Cells are washed, detached, and counted with a Coulter counter for the determination of cell growth.(Only for Reference)

激酶实验: H1-Antihistaminic Activity: The segments (1 cm) of isolated ileum from guinea pigs are suspended in an organ bath containing Tyrode solution (ventilation, 32 °C). The contractile responses to histamine (0.54 μM) are measured with an isotonic transducer. A set concentration of Chlorpheniramine is added in the organ bath 5 minutes before the addition of histamine. IC50 value of Chlorpheniramine is calculated by the probit methond.

体外活性: 在卵清蛋白活性皮肤过敏刺激的BALB/c小鼠和皮下注射组胺的ICR小鼠中,口服 Chlorpheniramine（10 mg/kg）能够抑制短期刮伤.在组胺诱导豚鼠中（ED50=0.17 mg/kg）,口服Chlorpheniramine能够抑制死亡.在大鼠中,Chlorpheniramine（20 mg/kg ）处理后,能够阻断产生快速眼动睡眠的组胺或胆碱机制.

体内活性: Chlorpheniramine能够抑制[3H]美吡拉敏与豚鼠皮层组胺H1受体结合（IC50=8.8 nM）。在MCF-7,MDA-MB 231和Ehrlich细胞中,Chlorpheniramine（250 μM）降低鸟氨酸脱羧酶mRNA翻译,抑制的增殖细胞增殖。在恶性疟原虫的CQS菌株（D6）（IC50=61.2uM）和MDR菌株（Dd2）（IC50=3.9uM）中,Chlorpheniramine具有抗疟活性。在伴刀豆球蛋白A诱导的鼠脾淋巴细胞中（IC50=33.4 μM）,Chlorpheniramine具有细胞毒性。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 50 mg/mL (127.92 mM)
DMSO : 100 mg/mL (255.84 mM)


关键字: Histamine Receptor | Chlorphenamine | Chlorpheniramine maleate | Chlorpheniramine Maleate | inhibit | NCI-C 55265 | Chlorpheniramine | Inhibitor | Chlorphenamine Maleate | NCI-C-55265

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相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | GPCR Compound Library | Anti-Cancer Approved Drug Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途