| Identification | Back Directory | [Name]
AMG8380 | [CAS]
1642112-32-0 | [Synonyms]
AMG8380 6-Quinolinesulfonamide, 1-(3'-chloro-2,5'-difluoro-5-methoxy[1,1'-biphenyl]-4-yl)-1,2-dihydro-N-3-isoxazolyl-2-oxo-, (1R)- | [Molecular Formula]
C25H16ClF2N3O5S | [MOL File]
1642112-32-0.mol | [Molecular Weight]
543.93 |
| Hazard Information | Back Directory | [Uses]
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]. | [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.
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| [IC 50]
hNav1.7: 0.907 μM (IC50); mNav1.7: 0.387 μM (IC50) | [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. DOI:10.1124/jpet.116.239590 |
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