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S87485

Ezutromid

源叶(MedMol) 98%
  • 英文名:
  • Ezutromid
  • 别名:
  • CAS号:
  • 945531-77-1
  • 分子式:
  • C19H15NO3S
  • 分子量:
  • 337.3923
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S87485-1mg 98% ¥229.50元 9 - - - EA 加入购物车
源叶(MedMol) S87485-2mg 98% ¥391.00元 8 - - - EA 加入购物车
源叶(MedMol) S87485-5mg 98% ¥660.00元 8 - - - EA 加入购物车
源叶(MedMol) S87485-10mg 98% ¥1062.50元 6 - - - EA 加入购物车
源叶(MedMol) S87485-25mg 98% ¥1870.00元 5 - - - EA 加入购物车
源叶(MedMol) S87485-50mg 98% ¥3300.00元 5 - - - EA 加入购物车
源叶(MedMol) S87485-100mg 98% ¥5400.00元 5 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM
  • 靶点: CYP1
  • 体外研究:
    Ezutromid induces increased levels of utrophin RNA in human muscle cells. Treatment of human DMD cells with Ezutromid lead to a 2-fold increase in utrophin protein levels at an optimal concentration of 0.3 uM after 3 days of treatment. Ezutromid was safe and well tolerated with plasma concentrations achieved suf cient to cause a 50% increase in concentrations of utrophin in cells. Ezutromid led to a 30% increase in Utrn mRNA level and resulted in a 2.0-fold increase in UTRN protein level
  • 体内研究:
    Note: You can dissolve the products in phosphate buffered saline (PBS), 0.1% Tween-20, 5% DMSO)
  • 参考文献:
    1. Chancellor DR, et al. Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of Duchenne muscular dystrophy. J Med Chem. 2011;54(9):3241-3250. 2. Chatzopoulou M, et al. Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-trans-Dihydro-1,2-diol Metabolites of the Utrophin Modulator Ezutromid. J Med Chem. 2020;63(5):2547-2556. 3. Tinsley JM et al. Daily treatment with SMTC1100, a novel small molecule utrophin upregulator, dramatically reduces the dystrophic symptoms in the mdx mouse. PLoS One. 2011 May 6;6(5):e19189. 4. Tinsley J et al. Safety, tolerability, and pharmacokinetics of SMT C1100, a 2-arylbenzoxazole utrophin modulator, following single- and multiple-dose administration to healthy male adult volunteers. J Clin Pharmacol. 2015 Jun;55(6):698-707. 5. Guiraud S et al. Second-generation compound for the modulation of utrophin in the therapy of DMD. Hum Mol Genet. 2015 Aug 1;24(15):4212-24.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.964 ml 14.82 ml 29.639 ml
    5 mM 0.593 ml 2.964 ml 5.928 ml
    10 mM 0.296 ml 1.482 ml 2.964 ml
    50 mM 0.059 ml 0.296 ml 0.593 ml
  • 注意:部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。
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