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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 g | ¥ 164 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 181 | 现货 |
产品描述 | Chlorpheniramine maleate (NCI-C55265) is a histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. |
靶点活性 | H1 receptor:12 nM |
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。 |
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. |
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) |
别名 | NCI-C55265, Chlorphenamine maleate, 马来酸氯苯那敏 |
分子量 | 390.87 |
分子式 | C20H23ClN2O4 |
CAS No. | 113-92-8 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 50 mg/mL (127.92 mM) DMSO: 100 mg/mL (255.84 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
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