Nav1.7-IN-23
Nav1.7-IN-23 is an orally active, selective NaV1.7 inhibitor. Nav1.7-IN-23 exhibits electrophysiological regulatory effects in mouse dorsal root ganglion neurons. Nav1.7-IN-23 can be used for the research of acute pain, chronic inflammatory pain and neuropathic pain.
For research use only. We do not sell to patients.
- CAS No.: 3138159-82-4
- Formula: C27H29ClN4O
- Molecular Weight:461.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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]|
Nav1.7 0.0098 μM (IC50) |
hNav1.1 2.59 μM (IC50) |
Nav1.2 2.19 μM (IC50) |
Nav1.3 3.09 μM (IC50) |
Nav1.4 6.56 μM (IC50) |
Nav1.5 5.49 μM (IC50) |
Nav1.6 7.69 μM (IC50) |
Nav1.8 9.18 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
1.76 μM
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Inhibition of hERG channels in HEK293T cells measured by manual whole-cell patch-clamp electrophysiology.
Inhibition of hERG channels in HEK293T cells measured by manual whole-cell patch-clamp electrophysiology.
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42503835 |
In Vitro
Nav1.7-IN-23 (Compound 56) potently inhibits NaV1.7 in cells with an IC50 of 0.0098 μM, and exhibits high selectivity over other isoforms including NaV1.1, NaV1.2, NaV1.3, NaV1.4, NaV1.5, NaV1.6 and NaV1.8[1].
Nav1.7-IN-23 inhibits hERG channels in HEK293T cells with an IC50 of 1.76 μM, which reduces the risk of hERG-related cardiotoxicity compared with WN2 and WN2-R[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
Nav1.7-IN-23 (100 mg/kg; p.o.; single dose) does not impair motor function in healthy mice, as measured by open field and rotarod tests[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (male)[1]
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Dosage:30 mg/kg
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Administration:p.o.; single dose
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Result:Increased paw withdrawal threshold to 1.13 g at 2 hours post-administration.
Elevated paw withdrawal thresholds across all measured time points from 0.5 to 3 hours post-administration.
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Animal Model:ICR mice (male, 18-22 g)[1]
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Dosage:100 mg/kg
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Administration:p.o.; single dose
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Result:Showed no significant difference in open field action distance relative to the saline control group.
Showed no significant difference in rotarod duration time relative to the saline control group.
Chemical Information
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CAS No. 3138159-82-4
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Molecular Weight 461.00
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Formula C27H29ClN4O
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SMILES
CN(C)CCNC(C[C@@H](C1=CC(Cl)=CC=C1)C2=CN(CC3=CN=CC=C3)C4=CC=CC=C24)=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-23 Related Classifications
HY-189066 Related Classifications
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