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AMG8380

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].

Product Specifications

CAS Number

1642112-32-0

UNSPSC

12352005

Target

Sodium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/amg8380.html

Solubility

10 mM in DMSO

Smiles

O=S(NC1=NOC=C1)(C2=CC(C=CC(N3C4=CC(F)=C(C=C4OC)C5=CC(Cl)=CC(F)=C5)=O)=C3C=C2)=O.[R]

Molecular Formula

C25H16ClF2N3O5S

Molecular Weight

543.93

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

Nav1.7

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