Ezutromid (Synonyms: BMN 195, SMT-C1100, VOX-C1100) |
Catalog No.GC19150 |
Ezutromid (SMT C1100) es un modulador de utrofina de benzoxazol activo por vÍa oral, primero en su clase, con un EC50 de 0,91 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 945531-77-1
Sample solution is provided at 25 µL, 10mM.
Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .In vitro: 1) SMT C1100 induces increased levels of utrophin RNA in human muscle cells.2) Treatment of human DMD cells with SMT C1100 lead to a 2-fold increase in utrophin protein levels at an optimal concentration of 0.3 uM after 3 days of treatment. 3) SMT C1100 wassafe and well tolerated with plasma concentrations achieved sufcient to cause a 50% increase in concentrations of utrophin in cells. 4) SMT C1100 led to a 30% increase in Utrn mRNA level and resulted in a 2.0-fold increase in UTRN protein level .In vivo: 1)The reference for administration is 50 mg/kg. 2) it was considered that no toxicity was determined for SMT C1100 administered by oral gavage to the mouse up to dose levels of 2000 mg/kg/day for 28 days.Note: You can dissolve the products in phosphate buffered saline (PBS), 0.1% Tween-20, 5% DMSO)
References:
[1]. 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.
[2]. 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.
[3]. 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.
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