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  • Chlorpheniramine Maleate
    • 马来酸氯苯那敏;Chlorphenamine maleate
    货号: abs816325
    CAS号: 113-92-8
    分子式: C16H19ClN2.C4H4O4
    分子量: 390.86
    产品说明书
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    货号-规格 货期 价格 数量
    abs816325-50mg 1-2周 ¥221.00
    - +
    abs816325-100mg 1-2周 ¥386.00
    - +
    abs816325-200mg 1-2周 ¥607.00
    - +
    abs816325-1g 1-2周 ¥1213.00
    - +
    大包装询价
    产品描述
    描述

    Chlorpheniramine Maleate是一种组胺H1受体拮抗剂,IC50为12 nM。Chlorpheniramine作用于豚鼠回肠,抑制组胺诱导的收缩,IC50为12 nM。 Chlorpheniramine作用于豚鼠大脑皮层,抑制[3H]mepyramine 结合到组胺组胺H1受体上,IC50为 8.8 nM。 Chlorpheniramine抑制 MCF-7, MDA-MB 231,和Ehrlich细胞增殖,这种作用存在剂量反应性,且250 μM时,显著降低鸟氨酸脱羧酶mRNA 翻译,降低50%-70%。

    纯度
    >98%
    储存/保存方法
    -20°C
    基本信息
    别名
    马来酸氯苯那敏;Chlorphenamine maleate
    外观
    白色结晶性粉末
    可溶性/溶解性
    DMSO 70 mg/mL
    生物活性
    靶点
    Histamine H1 receptor
    In vitro(体外研究)
    Chlorpheniramine inhibits the mepyramine binding to the histamine H1 receptor in guinea pig cortex with IC50 of 8.8 nM. Chlorpheniramine inhibits the proliferation of MCF-7, MDA-MB 231, and Ehrlich cells in a dose-response manner, and significantly reduces the ornithine decarboxylase mRNA translation by 50%-70% at the 250 μM. Chlorpheniramine displaces of pyrilamine from human histamine receptor subtype 1 expressed in CHO cells with IC50 of 66 nM. Chlorpheniramine displays antimalarial activity against CQS strain (D6) and MDR strain (Dd2) of P. falciparum with IC50 of 61.2 uM and 3.9 uM, respectively. Chlorpheniramine displays cytotoxicity against the proliferation of concanavalin A-induced murine splenic lymphocytes with IC50 of 33.4 μM. Chlorpheniramine treatment in human salivary gland cells more significantly inhibits the histamine-induced i increase in a concentration-dependent manner with IC50 of 128 nM than that of carbachol-induced i increase with an IC50 of 43.9 μM.
    In vivo(体内研究)
    Oral administration of Chlorpheniramine inhibits histamine-induced mortality in guinea pigs with an ED50 of 0.17 mg/kg. Oral administration of Chlorpheniramine (10 mg/kg) significantly inhibits short-duration scratching in BALB/c mice stimulated by ovalbumin active cutaneous anaphylaxis and in ICR mice subcutaneously injected with histamine, but not long-duration scratching seen in NC/Nga mice, in contrast to that of dexamethasone or tacrolimus. Administration of Chlorpheniramine (20 mg/kg) significantly abolishes the increase in REM sleep in rats induced by immobilization stress due to the blockage of the histaminergic and cholinergic mechanisms generating REM sleep.
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