Soticlestat (TAK-935; OV935) 是一种首创的，有效的，选择性的，具有口服活性的胆固醇 24-羟化酶 (cholesterol 24-hydroxylase, CYP46A1) 抑制剂。Soticlestat 可用于癫痫综合征的研究。
货号:ajcx35212
CAS:1429505-03-2
分子式:C23H23N3O2
分子量：373.45
溶解度:DMSO : 100 mg/mL (267.77 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.