Synonyms: compound 1 [PMID: 33682420] | compound 4 [PMID: 31012583] | GDC0276
Compound class:
Synthetic organic
Comment: GDC-0276 is a voltage-gated sodium ion channel subtype 1.7 (NaV1.7) modulator [1-2]. It was developed as a non-opioid analgesic. It binds to the channel's voltage sensor in domain IV.
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Bioactivity Comments |
Inhibits veratridine-induced Nav1.7 current in HEK293 cells, with an IC50 of 40 nM using a sodium influx assay [2]. In a whole cell voltage-clamp assay the IC50 for inhibition of Nav1.7 current is 0.4 nM. |