| Bioactivity | Soticlestat (TAK-935; OV935) is a first-in-class, potent, selective, and orally active cholesterol 24-hydroxylase (CH24H) inhibitor. Soticlestat has the potential for epilepsy syndromes research[1][2]. | ||||||||||||
| Invitro | Soticlestat inhibits the catalytic activity of human cholesterol 24-hydroxylase (CH24H) in a concentration-dependent manner with an IC50 of 4.5 nM[1]. | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | Soticlestat | ||||||||||||
| CAS | 1429505-03-2 | ||||||||||||
| Formula | C23H23N3O2 | ||||||||||||
| Molar Mass | 373.45 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |