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1642112-32-0

1642112-32-0 Structure

1642112-32-0 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[Boiling point ]

752.0±70.0 °C(Predicted)
[density ]

1.527±0.06 g/cm3(Predicted)
[pka]

4.89±0.20(Predicted)
Hazard InformationBack 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.
[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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