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  • Phenothiazine
    • 吩噻嗪
    货号: abs813778
    CAS号: 92-84-2
    分子式: C12H9NS
    分子量: 199.27
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs813778-25mg 1-2周 ¥524.00
    - +
    abs813778-50mg 1-2周 ¥834.00
    - +
    abs813778-100mg 1-2周 ¥1233.00
    - +
    abs813778-200mg 1-2周 ¥1542.00
    - +
    大包装询价
    产品描述
    描述

    Phenothiazine is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain.

    纯度
    >98%
    储存/保存方法
    -20°C
    基本信息
    别名
    吩噻嗪
    外观
    黄色至绿灰色粉末或片状结晶
    可溶性/溶解性
    DMSO :38 mg/mL (190.7 mM)
    生物活性
    靶点
    D2 receptor
    In vitro(体外研究)
    Phenothiazines mostly substitutes at position 10 with the dialkylaminoalkyl groups and additionally at position 2 with small groups exhibit valuable activities such as neuroleptic, antiemetic, antihistaminic, antipuritic, analgesic and antihelmintic. 2-trifluoromethyl-10-(4-aminobutyl)phenothiazine inhibits S. cerevisiae strains and T. mentagrophites with MIC of 0.4 μg/mL and 1.5 μg/mL, respectively. 10-carbamoylalkylphenothiazines shows significant activities against Gram-positive Bacillus subtilis with MIC’s in the range of 7.8 μg/mL–30 μg/mL. The tetracyclic phenothiazines (modified with the naphthoquinone ring) shows significant actibacterial activity against S. aureus with the MIC50 of 12.5 μg/mL. Phenothiazines with the butylene linker are more effective than with the propylene linker, the 2-chloro-10-chloroethylureidobutyl derivative giving GI50 of 1.4 μM and 1.6 μM against 4 leukemia cell lines and 7 colon cancer cell lines. 10-Amino(hydroxy)propylphenothiazines (5 μM) induces a marked G2/M phase of cell-cycle arrest followed by cell death in human transformed WI38VA cells after 2-day incubation. Phenothiazine drugs undergo extensive metabolism in the body before being excreted, mainly ring hydroxylation, ring sulphoxidation, N-demethylation, N-oxidation, sulphate and glucuronide conjugation. Phenothiazines have considerably lower binding affinities to α2-adrenoceptors than to dopamine D2 receptors and al-adrenoceptors. Phenothiazines have significant in vitro activity against susceptible, polydrug- and multidrug-resistant strains of M. tuberculosis, as well as enhancing the activity of some agents employed for first-line treatment.
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