AMG8379 is a potent, orally active and selective sulfonamide antagonist of thevoltage-gatedsodium channelNaV1.7, withIC₅₀s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC₅₀of 3.1 nM^[1].

AMG8379 is 100 to 1000-fold selective over other NaV family members, including NaV1.4 expressed in muscle and NaV1.5 expressed in heart, as well as TTX-resistant NaV channels in DRG neurons^[1].
The IC₅₀for AMG8379 inhibition of C-fiber spiking based on the level of firing in NaV1.7 KO mice representing complete pharmacological block of the NaV1.7-component of this assay is calculated. In this manner, the IC₅₀for AMG8379 block is 47.0 ± 8.1 nM^[1].

AMG8379 (30-100 mg/kg; p.o.) inhibits Capsaicin-induced nociceptive behavior^[1].

543.93

C₂₅H₁₆ClF₂N₃O₅S

1642112-31-9

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