AMG8379
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.
For research use only. We do not sell to patients.
- CAS No.: 1642112-31-9
- Formula: C25H16ClF2N3O5S
- Molecular Weight:543.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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hNav1.7 8.5 nM (IC50) |
mNav1.7 18.6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>14 μM
Compound: 15; AMG8379
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Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
>14 μM
Compound: 15; AMG8379
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Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
>14 μM
Compound: 15; AMG8379
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Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
>14 μM
Compound: 15; AMG8379
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Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
AMG8379 is 100 to 1000-fold selective over other NaV family members, including NaV1.4 expressed in muscle and NaV1.5 expressed in heart, as well as TTX-resistant NaV channels in DRG neurons[1].
The IC50 for AMG8379 inhibition of C-fiber spiking based on the level of firing in NaV1.7 KO mice representing complete pharmacological block of the NaV1.7-component of this assay is calculated. In this manner, the IC50 for AMG8379 block is 47.0 ± 8.1 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 male mice[1]
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Dosage:30 or 100 mg/kg body weight
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Administration:Oral
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Result:Showed a dose-dependent reduction in overall nociceptive behavior.
Chemical Information
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CAS No. 1642112-31-9
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Molecular Weight 543.93
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Formula C25H16ClF2N3O5S
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SMILES
O=S(NC1=NOC=C1)(C2=CC(C=CC(N3C4=C(OC)C=C(C(F)=C4)C5=CC(Cl)=CC(F)=C5)=O)=C3C=C2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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