| Identification | Back Directory | [Name]
(P)-1-(3'-Chloro-2,5'-Difluoro-5-Methoxy-4-Biphenylyl)-N-3-Isoxazolyl-2-Oxo-1,2-Dihydro-6-Quinolinesulfonamide | [CAS]
1642112-31-9 | [Synonyms]
AMG8379
(P)-1-(3'-Chloro-2,5'-Difluoro-5-Methoxy-4-Biphenylyl)-N-3-Isoxazolyl-2-Oxo-1,2-Dihydro-6-Quinolinesulfonamide | [Molecular Formula]
C25H16ClF2N3O5S | [MDL Number]
MFCD34567154 | [MOL File]
1642112-31-9.mol | [Molecular Weight]
543.93 |
| Hazard Information | Back Directory | [Description]
AMG8379 is a potent and selective antagonist of the voltage-gated sodium channel NaV1.7. | [Uses]
AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s 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 IC50 of 3.1 nM[1]. | [in vivo]
AMG8379 (30-100 mg/kg; p.o.) inhibits Capsaicin-induced nociceptive behavior[1]. | Animal Model: | CD-1 male mice[1] | | Dosage: | 30 or 100 mg/kg body weight | | Administration: | Oral | | Result: | Showed a dose-dependent reduction in overall nociceptive behavior.
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| [IC 50]
hNav1.7: 8.5 nM (IC50); mNav1.7: 18.6 nM (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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