Dataset Information

NBI-921352, a first-in-class, Na_V1.6 selective, sodium channel inhibitor that prevents seizures in Scn8a gain-of-function mice, and wild-type mice and rats.

ABSTRACT: NBI-921352 (formerly XEN901) is a novel sodium channel inhibitor designed to specifically target Na_V1.6 channels. Such a molecule provides a precision-medicine approach to target SCN8A-related epilepsy syndromes (SCN8A-RES), where gain-of-function (GoF) mutations lead to excess Na_V1.6 sodium current, or other indications where Na_V1.6 mediated hyper-excitability contributes to disease (Gardella and Møller, 2019; Johannesen et al., 2019; Veeramah et al., 2012). NBI-921352 is a potent inhibitor of Na_V1.6 (IC₅₀0.051 µM), with exquisite selectivity over other sodium channel isoforms (selectivity ratios of 756 X for Na_V1.1, 134 X for Na_V1.2, 276 X for Na_V1.7, and >583 Xfor Na_V1.3, Na<

SUBMITTER: Johnson JP

PROVIDER: S-EPMC8903829 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature

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Dataset Information

NBI-921352, a first-in-class, Na_V1.6 selective, sodium channel inhibitor that prevents seizures in Scn8a gain-of-function mice, and wild-type mice and rats.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Dataset Information

NBI-921352, a first-in-class, NaV1.6 selective, sodium channel inhibitor that prevents seizures in Scn8a gain-of-function mice, and wild-type mice and rats.

OmicsDI is part of the ELIXIR infrastructure

Tweets

NBI-921352, a first-in-class, Na_V1.6 selective, sodium channel inhibitor that prevents seizures in Scn8a gain-of-function mice, and wild-type mice and rats.