Nav1.7-IN-3
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Based on 1 Customer Validation
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
For research use only. We do not sell to patients.
- Purity: 98.21%
- CAS No.: 1788872-06-9
- Formula: C17H20ClFN4O2S2
- Molecular Weight:430.95
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Biological Activity
Description
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration[1].
IC50 & Target[1]
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Nav1.7 8 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
8 nM
Compound: 5
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Inhibition of 50% inactivated human Nav1.7alpha expressed in HEK293 cells at holding potential of -60 mV incubated for 5 mins measured at 10 secs interval by PatchXpress electrophysiology assay
Inhibition of 50% inactivated human Nav1.7alpha expressed in HEK293 cells at holding potential of -60 mV incubated for 5 mins measured at 10 secs interval by PatchXpress electrophysiology assay
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[PMID: 28389149] |
| HEK293 | IC50 |
>30000 nM
Compound: 5
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Inhibition of 50% inactivated human Nav1.5alpha expressed in HEK293 cells at holding potential of -60 mV incubated for 5 mins measured at 10 secs interval by PatchXpress electrophysiology assay
Inhibition of 50% inactivated human Nav1.5alpha expressed in HEK293 cells at holding potential of -60 mV incubated for 5 mins measured at 10 secs interval by PatchXpress electrophysiology assay
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[PMID: 28389149] |
| HEK293 | IC50 |
2.2 nM
Compound: 3
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Inhibition of human Nav1.5 inactivated state form expressed in HEK293 cells at -60 mV holding potential by by automated patch clamp electrophysiology assay
Inhibition of human Nav1.5 inactivated state form expressed in HEK293 cells at -60 mV holding potential by by automated patch clamp electrophysiology assay
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[PMID: 28818462] |
| HEK293 | IC50 |
>30000 nM
Compound: 3
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Inhibition of human Nav1.5 inactivated state form expressed in HEK293 cells at -50 mV holding potential by by automated patch clamp electrophysiology assay
Inhibition of human Nav1.5 inactivated state form expressed in HEK293 cells at -50 mV holding potential by by automated patch clamp electrophysiology assay
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[PMID: 28818462] |
| HEK293 | IC50 |
3.9 nM
Compound: 2
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Inhibition of recombinant mouse Nav1.7 expressed in HEK293 cells at -70 mV holding potential by patch clamp electrophysiology method
Inhibition of recombinant mouse Nav1.7 expressed in HEK293 cells at -70 mV holding potential by patch clamp electrophysiology method
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[PMID: 30576602] |
In Vivo
Nav1.7-IN-3 (compound 5) shows excellent potency, selectivity, behavioral efficacy in a rodent pain model (30 mg/kg, oral, 35 minutes), and efficacy in a mouse itch model (30 mg/kg, oral, 30 minutes)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 male mice (n=8/group, 25-30g)
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Dosage:1, 3, and 10 mg/kg
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Administration:Oral (0-35 mintues)
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Result:Nav1.7-IN-3 demonstrates statistically significant, dose-dependent reversal of these effects in the acute phase of the experiment (0-5 min period post formalin injection) and the tonic phase of the experiment (20-35 min period post formalin injection) with full reversal of formalin effects in the tonic phase[1]
Chemical Information
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CAS No. 1788872-06-9
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Appearance Solid
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Molecular Weight 430.95
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Formula C17H20ClFN4O2S2
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Color White to off-white
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SMILES
FC1=C(S(=O)(NC2=NC=CS2)=O)C=C(Cl)C(NCC34CCCN3CCC4)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : < 1 mg/mL (insoluble or slightly soluble)
View the Complete Stock Solution Preparation Table
Purity & Documentation
Select Batch:
Purity:
99.98%
Assay:
99.98%
ee.:
99.98%
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
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