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 No.: 1642113-59-4
- Formula: C27H19F3N4O4S
- Molecular Weight:552.52
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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
All Histamine Receptor Isoforms
More
Biological Activity
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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
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[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
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[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
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[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
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[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
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[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
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[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
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[PMID: 28324649] |
Chemical Information
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CAS No. 1642113-59-4
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Molecular Weight 552.52
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Formula C27H19F3N4O4S
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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
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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)
AM-0466 Related Classifications
HY-135495 Related Classifications
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