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Art. -Nr.: HY-135495

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AM-0466

AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing.

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CAS. Nr.: 1642113-59-4
Formel: C₂₇H₁₉F₃N₄O₄S
Molecular Weight:552.52

Speicherung:

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

Data Sheet (272 KB)

AM-0466 Chemical Structure

CAS. Nr.: 1642113-59-4

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- Cellular Effect
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>30 μM Compound: 39	Inhibition of human Nav1.5 expressed in HEK293 cells incubated for 3 to 5 mins at -50 mV holding potential by patchXpress electrophysiology assay Inhibition of human Nav1.5 expressed in HEK293 cells incubated for 3 to 5 mins at -50 mV holding potential by patchXpress electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	>42.5 μM Compound: 39	Inhibition of human Nav1.1 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay Inhibition of human Nav1.1 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	>42.5 μM Compound: 39	Inhibition of human Nav1.4 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay Inhibition of human Nav1.4 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	>42.5 μM Compound: 39	Inhibition of human Nav1.5 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay Inhibition of human Nav1.5 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	0.005 μM Compound: 2	Inhibition of slow inactivated human NaV1.7 expressed in HEK293 cells at -20 mV holding potential after 5 mins by IonWorks electrophysiology method Inhibition of slow inactivated human NaV1.7 expressed in HEK293 cells at -20 mV holding potential after 5 mins by IonWorks electrophysiology method	[PMID: 28684121]
HEK293	IC₅₀	0.006 μM Compound: 39	Inhibition of human Nav1.7 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay Inhibition of human Nav1.7 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	0.02 μM Compound: 2	Inhibition of human NaV1.7 expressed in HEK293 cells at -125 mV holding potential yielding 20 to 50% inactivation after 3 to 5 mins by PatchXpress automated electrophysiology method Inhibition of human NaV1.7 expressed in HEK293 cells at -125 mV holding potential yielding 20 to 50% inactivation after 3 to 5 mins by PatchXpress automated electrophysiology method	[PMID: 28684121]
HEK293	IC₅₀	0.021 μM Compound: 39	Inhibition of human Nav1.7 expressed in HEK293 cells at holding potential yielding 20 to 50% inactivation measured after 3 to 5 mins by patchXpress electrophysiology assay Inhibition of human Nav1.7 expressed in HEK293 cells at holding potential yielding 20 to 50% inactivation measured after 3 to 5 mins by patchXpress electrophysiology assay	[PMID: 28324649]
HEK293	IC₅₀	0.65 μM Compound: 39	Inhibition of human Nav1.6 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay Inhibition of human Nav1.6 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology assay	[PMID: 28324649]

Chemical Information

CAS. Nr. 1642113-59-4
Molecular Weight 552.52
Formel C₂₇H₁₉F₃N₄O₄S
SMILES

O=C1N(C2=C(OC)C=C(C=C2)C3=CC(C(F)(F)F)=CC=C3)C4=CC=C(S(=O)(NC5=NC=CC=N5)=O)C=C4C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 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)
Handling Instructions (2659 KB)

Verweise

[1]. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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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Biologische Aktivität
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Chemical Information
Reinheit & Dokumentation
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AM-0466

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

AM-0466 Related Classifications

HY-135495 Related Classifications