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.

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^[4][5].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Note: You can dissolve the products in phosphate buffered saline (PBS), 0.1% Tween-20, 5% DMSO)

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Note: You can dissolve the products in phosphate buffered saline (PBS), 0.1% Tween-20, 5% DMSO)

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . 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.  [Content Brief]

  . 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.  [Content Brief]

  . 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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]