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Chemical Structure : NBI-921352
Catalog No.: PC-72850Not For Human Use, Lab Use Only.
NBI-921352 (XEN901, NBI 921352) is a potent, highly selective, orally active inhibitor of NaV1.6 with IC50 of 51 nM (hNaV1.6 channel currents inhibition).
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NBI-921352 (XEN901, NBI 921352) is a potent, highly selective, orally active inhibitor of NaV1.6 with IC50 of 51 nM (hNaV1.6 channel currents inhibition).
NBI-921352 displays selectivity ratios for hNaV1.6 versus the other hNaV isoforms (IC50 hNaV1.X / IC50 hNaV1.6) of 756 (NaV1.1), 134 (NaV1.2), 276 (NaV1.7) and >583 (NaV1.3, NaV1.4, NaV1.5).
NBI-921352 is a state-dependent inhibitor, preferentially inhibiting inactivatedchannels.
NBI-921352 demonstrated action-potential firing in glutamatergic excitatory pyramidal neurons, while sparing fast-spiking inhibitory interneurons, where NaV1.1 predominates.
Oral administration of NBI-921352 prevented electrically induced seizures in a Scn8a GoF mouse, as well as in wild-type mouse and rat seizure models.
NBI-921352 is more potent than three commonly sodium channel inhibitor anti-seizure medicines (carbamazepine, phenytoin, and lacosamide).
| M.Wt | 460.586 | |
| Formula | C22H25FN4O2S2 | |
| Appearance | Solid | |
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1. J P Johnson, et al. Elife. 2022 Mar 2;11:e72468.
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