Soticlestat (Synonyms: OV935, TAK-935) |
رقم الكتالوجGC63199 |
Soticlestat (TAK-935 ؛ OV935) هو مثبط الكوليسترول 24-هيدروكسيلاز (CH24H) الأول في فئته ، والقوي ، والانتقائي ، والنشط عن طريق الفم
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Cas No.: 1429505-03-2
Sample solution is provided at 25 µL, 10mM.
Soticlestat (TAK-935; OV935) is a first-in-class, potent, selective, and orally active cholesterol 24-hydroxylase (CYP46A1) inhibitor. Soticlestat has the potential for epilepsy syndromes research[1][2].
Soticlestat inhibits the catalytic activity of human cholesterol 24-hydroxylase (CH24H) in a concentration-dependent manner with an IC50 of 4.5 nM[1].
Soticlestat treatment lowers brain 24S-hydroxycholesterol in a dose-dependent manner and substantially reduceds premature deaths of APP/PS1-Tg mice at a dose lowering brain 24S-hydroxycholesterol by approximately 50%. Soticlestat can suppress potassium-evoked extracellular glutamate elevations in the hippocampus[1].
[1]. Toshiya Nishi, et al. Soticlestat, a novel cholesterol 24-hydroxylase inhibitor shows a therapeutic potential for neural hyperexcitation in mice. Sci Rep. 2020 Oct 13;10(1):17081.
[2]. Krista Eschbach, et al. Stiripentol for the treatment of seizures in Dravet syndrome. Expert Rev Clin Pharmacol. 2019 May;12(5):379-388.
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