AMG8380

Names

[ Name ]:
AMG8380

Biological Activity

[Description]:

AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Research Areas >> Neurological Disease

[In Vivo]

Animal Model: C57Bl/6 male mice[1] Dosage: 100 mg/kg Administration: oral Result: Failed to show a statistically significant effect on scratching behavior.

[References]

[1]. Kornecook TJ, et al. Pharmacologic Characterization of AMG8379, a Potent and Selective Small Molecule Sulfonamide Antagonist of the Voltage-Gated Sodium Channel NaV1.7. J Pharmacol Exp Ther. 2017 Jul;362(1):146-160.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₁₆ClF₂N₃O₅S

[ Molecular Weight ]:
543.93

Related Compounds

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