Nav1.7-IN-8
Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain.
For research use only. We do not sell to patients.
- CAS No.: 1432913-44-4
- Formula: C21H12ClF2N5O4S2
- Molecular Weight:535.93
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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
Description
IC50 & Target
[1]|
CYP2C9 0.17 μM (IC50) |
Nav1.7 |
CYP3A4 0.077 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.4 nM
Compound: 3
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Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
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[PMID: 26985315] |
| HEK293 | IC50 |
0.4 nM
Compound: 3
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Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage clamp analysis
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage clamp analysis
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[PMID: 26985315] |
| HEK293 | IC50 |
11 nM
Compound: 3
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Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
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[PMID: 26985315] |
| HEK293 | IC50 |
1380 nM
Compound: 3
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Inhibition of full length human Nav1.5 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.5 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
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[PMID: 26985315] |
| HEK293 | IC50 |
3080 nM
Compound: 3
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Inhibition of full length human Nav1.1 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -40 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.1 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -40 mV by automated voltage clamp analysis
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[PMID: 26985315] |
| HEK293 | IC50 |
4.2 nM
Compound: 3
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Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
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[PMID: 26985315] |
In Vitro
Nav1.7-IN-8 plasma protein binding is very high in rat with a free fraction of ∼1.1 %[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
. Nav1.7-IN-8 (10~100 mpk, i.p.; 2 days) displays a dose-dependent reduction of the pain response[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:0~100 mpk
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Administration:I.p.; 1 hour
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Result:Showed a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produced a substantial inhibition of the pain response.
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Animal Model:Mice[1]
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Dosage:10~100 mpk
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Administration:I.p.; 2 days
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Result:Displayed a dose-dependent reduction of the pain response.
Chemical Information
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CAS No. 1432913-44-4
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Molecular Weight 535.93
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Formula C21H12ClF2N5O4S2
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SMILES
O=S(NC1=NC=NS1)(C2=C(F)C=C(OC3=C(C4=CC=C5ON=C(C5=C4)N)C=C(Cl)C=C3)C(F)=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)
Nav1.7-IN-8 Related Classifications
HY-141547 Related Classifications
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