LTGO-33 is a potent and selective inhibitor of voltage-gated sodium channel NaV1.8. LTGO-33, with its potency in the nanomolar range, selectively inhibits NaV1.8 over 600 times more than human NaV1.1-NaV1.7 and NaV1.9. Its inhibition is not dependent on the state of the channels and displays consistent potency against both closed and inactivated conformations. LTGO-33 holds promise for research in pain disorders.