首页 产品中心
  • Ambrisentan

    • 安倍生坦;BSF 208075;LU 208075
    货号: abs813296
    CAS号: 177036-94-1
    分子式: C22H22N2O4
    分子量: 378.42
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs813296-5mg 1-2周 ¥522.00
    - +
    abs813296-10mg 1-2周 ¥1345.00
    - +
    abs813296-20mg 1-2周 ¥2084.00
    - +
    abs813296-50mg 1-2周 ¥2305.00
    - +
    大包装询价
    产品描述
    描述

    Ambrisentan是一种高选择性的内皮素-1A型受体拮抗剂,IC50为18 nM,用于治疗肺动脉高血压(PAH)。

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    安倍生坦;BSF 208075;LU 208075
    可溶性/溶解性
    Ethanol :21 mg/mL (55.5 mM)
    DMSO :71 mg/mL (187.6 mM)
    生物活性
    靶点
    ET-A
    In vitro(体外研究)
    Ambrisentan only increases intracellular calcein fluorescence in P388/dx cells at concentrations above 100 μM and in L-MDR1 cells not at all indicating negligible P-gp inhibition. Ambrisentan inhibits specific ET-1 binding in these tissues in a concentration-dependent manner. Ambrisentan undergoes oxidative metabolism mainly by cytochrome P450 (CYP) 3A4 and to a lesser extent by CYP3A5 and CYP2C19. Ambrisentan is not only a strong inducer of CYP3A4, but also of ABCB1 and ABCG2. Ambrisentan also has a concentration-dependent effect on PXR activity, but because plateau effects are not reached, an EC50-value could not be calculated. Ambrisentan inhibits specific ET-1 binding in a concentration-dependent manner at nanomolar ranges of IC50. Ambrisentan significantly increases the dissociation constant for bladder ET-1 binding without affecting maximal number of binding sites (Bmax). Ambrisentan seem to bind to bladder ET-1 receptor in a competitive and reversible manner. Ambrisentan is an effective and safe treatment which is a valuable addition to the armamentarium against PAH. Ambrisentan offers a relative lack of drug interactions, once daily dosing and reassuring liver safety, offering safety and convenience advantages over bosentan.
    In vivo(体内研究)
    In the Ambrisentan group, hepatic hydroxyproline content is significantly lower than in the control group (18.0 μg/g±6.1 μg/g vs 33.9 μg/g±13.5 μg/g liver, respectively, P=0.014). Hepatic fibrosis estimated by Sirius red staining and areas positive for α-smooth muscle actin, indicative of activated hepatic stellate cells, are also significantly lower in the Ambrisentan group (0.46%±0.18% vs 1.11%±0.28%, respectively, P=0.0003; and 0.12%±0.08% vs 0.25%±0.11%, respectively, P=0.047). Moreover, hepatic RNA expression levels of procollagen-1 and tissue inhibitor of metalloproteinase-1 (TIMP-1) are significantly lower by 60% and 45%, respectively, in the Ambrisentan group. Inflammation, steatosis, and endothelin-related mRNA expression in the liver are not significantly different between the groups. Ambrisentan attenuates the progression of hepatic fibrosis by inhibiting hepatic stellate cell activation and reducing procollagen-1 and TIMP-1 gene expression. Ambrisentan did not affect inflammation or steatosis.
    参考文献
    参考文献
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
    • 实验方法 实验条件
      0张,还能上传 8 提交
          提示: 尊敬的客户您好,如果您对我们的产品有什么疑问或想要了解的,可以点击“我要咨询”按钮填写您的疑问。
          提交不成功?请联系info@absin.cn。
          我要咨询

      促销资讯 更多

        订购信息
        您可以从我们的授权经销商处购买absin产品或获得技术支持。若要查看您所在地区的经销商,请从以下的下拉列表中选择。
        GO
        • 0