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Cat. No.: HY-108425

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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.

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CAS No.: 1642112-31-9
Formule: C₂₅H₁₆ClF₂N₃O₅S
Masse moléculaire:543.93

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

AMG8379 Chemical Structure

CAS No.: 1642112-31-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

IC₅₀ & Target

hNa_v1.7

8.5 nM (IC₅₀)

mNa_v1.7

18.6 nM (IC₅₀)

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Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>14 μM Compound: 15; AMG8379	Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	>14 μM Compound: 15; AMG8379	Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	>14 μM Compound: 15; AMG8379	Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	>14 μM Compound: 15; AMG8379	Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]

In Vitro

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.

In Vivo

AMG8379 (30-100 mg/kg; p.o.) inhibits Capsaicin-induced nociceptive behavior^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS No. 1642112-31-9
Masse moléculaire 543.93
Formule C₂₅H₁₆ClF₂N₃O₅S
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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AMG8379

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