首页 产品中心
  • JNJ-1661010

    • Takeda-25
    货号: abs813688
    CAS号: 681136-29-8
    分子式: C19H19N5OS
    分子量: 365.45
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs813688-10mg 1-2周 ¥945.00
    - +
    abs813688-25mg 1-2周 ¥2091.00
    - +
    abs813688-50mg 1-2周 ¥3251.00
    - +
    abs813688-100mg 1-2周 ¥5204.00
    - +
    大包装询价
    产品描述
    描述

    JNJ-1661010 is a potent and selective FAAH inhibitor with IC50 of 10 nM (rat) and 12 nM (human), exhibits >100-fold selectivity for FAAH-1 when compared to FAAH-2.

    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
    Takeda-25
    外观
    白色粉末
    可溶性/溶解性
    Ethanol :3.7 mg/mL (10 mM)

    DMSO :36.6 mg/mL (100 mM)
    生物活性
    靶点
    FAAH (rat),FAAH (human)
    In vitro(体外研究)
    FAAH preincubated with JNJ-1661010 suggests a slow reversibility of the interaction between the JNJ-1661010 and the active site, which is accelerated at higher temperatures. JNJ-1661010 is a covalent, mechanism-based substrate inhibitor as examined by LC-ESI-MS. JNJ-1661010 docks with the phenylthiadiazole in the hydrophobic tunnel and the phenylurea in the hydrophilic pocket of FAAH.
    In vivo(体内研究)
    JNJ-1661010 (20 mg/kg i.p.) inhibits FAAH by at least 85% for up to 4 h after dosing, resulting accumulation of lipid ethanolamides in rat brain. JNJ-1661010 dose-dependently reverses the tactile allodynia with a maximum efficacy of approximately 90% at 30 min postdose in both Mild Thermal Injury (MTI) mice and rat model. JNJ-1661010 (20 mg/kg) reverses tactile allodynia by 60.8% at 30 min in rat spinal nerve ligation injury model. JNJ-1661010 (50 mg/kg i.p.) shows a significant attenuation of the hyperalgesia at 30 min postdose in rat carrageenan model of inflammatory pain. Rats dosed with JNJ-1661010 (20 mg/kg i.p.) has a plasma Cmax of 26.9 μM at the Tmax of 0.75 h and a Cmax in the brain of 6.04 μM at the Tmax of 2 h. JNJ-1661010 (20 mg/kg i.p.) inhibits brain FAAH and elevates AEA level in brain tissue in rat.
    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“我要提问”按钮填写您的疑问。
          提交不成功?请联系info@absin.cn。
          我要提问

      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