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  • Desloratadine
    • 脱羧氯雷他定;地氯雷他定;Sch34117
    货号: abs813592
    CAS号: 100643-71-8
    分子式: C19H19ClN2
    分子量: 310.82
    产品说明书
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    货号-规格 货期 价格 数量
    abs813592-25mg 1-2周 ¥563.00
    - +
    abs813592-50mg 1-2周 ¥607.00
    - +
    abs813592-100mg 1-2周 ¥1544.00
    - +
    abs813592-200mg 1-2周 ¥2337.00
    - +
    大包装询价
    产品描述
    描述

    Desloratadine is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.

    纯度
    >98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    脱羧氯雷他定;地氯雷他定;Sch34117
    外观
    白色或类白色粉末
    可溶性/溶解性
    Ethanol :31.1 mg/mL (100 mM)

    DMSO :6.2 mg/mL (20 mM)
    生物活性
    靶点
    Histamine H1 receptor
    In vitro(体外研究)
    Desloratadine is a competitive antagonist of carbachol-induced contractions in isolated rabbit iris smooth muscle with pA2 of 6.67. Desloratadine binds to the human H1 receptor with Ki value of 0.87 nM in displacing tritiated mepyramine. Desloratadine (100 nM to 10 μM) inhibits both IgE-mediated and non–IgE-mediated generation of the cytokines IL-4 and IL-13 by human basophils. Desloratadine (300 nM to 100 μM) inhibits both IgE and non–IgE-mediated histamine release from human peripheral blood basophils. Desloratadine (0.1 μM to 10 μM) is also shown to inhibit platelet-activating factor-induced eosinophil chemotaxis and TNF-α-induced eosinophil adhesion in eosinophils obtained from patients with allergic rhinitis or allergic asthma. Desloratadine (1 μM-10 μM) dose-dependently inhibits the release of histamine and LTC4 from human basophils. Desloratadine (0.1 μM-10 μM) dose-dependently inhibits IL-13 secretion from basophils activated with IL-3 and PMA from human basophils. Desloratadine (10 μM) pretreatment results in a substantial decrease of the induced cytokine message in cultured basophils. Desloratadine (10 μM) pretreatment causes approximately an 80% reduction in the IL-4 message accumulated with anti-IgE activation in cultured basophils. Desloratadine (10 μM) also inhibits the histamine and IL-4 protein secreted into the supernatants of cultured basophils. Desloratadine binds to the human histamine H1 receptor expressed in CHO cells with Kd of 1.1 nM. Desloratadine is 52, 57, 194, and 153 times more potent than cetirizine, ebastine, fexofenadine, and loratadine, respectively, in competition-binding studies.
    In vivo(体内研究)
    Desloratadine (1 mg/mL, 3 mg/mL and 10 mg/mL) induces a dose-dependent and long lasting mydriasis in the guinea-pig in vivo. Desloratadine inhibits histamine-induced paw edema with ED50 of 0.15 mg/kg in mice. Desloratadine inhibits an increase in microvascular permeability in response to a histamine challenge to the upper airway of guinea pigs with ED50 of 0.9 μg. Desloratadine (5 mg/kg) causes inhibition of oxotremorine-induced tremor by disrupting blood-brain barrier in conscious mice. Desloratadine (1.0 mg/kg) significantly inhibits oxotremorine-induced (0.00125 mg/kg, 0.0025 mg/kg, and 0.02 mg/kg) decreases in dP/dt indicated by a shift in the dose-response curve to the right in the pithed rat. Desloratadine (1.0 mg/kg) significantly inhibits oxotremorine-induced (0.00125 mg/kg, 0.0025 mg/kg, and 0.02 mg/kg) decreases in dP/dt indicated by a shift in the dose-response curve to the right in the pithed rat.
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