AMG8379
AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM.
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- CAS 番号: 1642112-31-9
- 分子式: C25H16ClF2N3O5S
- 分子量:543.93
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
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hNav1.7 8.5 nM (IC50) |
mNav1.7 18.6 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>14 μM
Compound: 15; AMG8379
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Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
>14 μM
Compound: 15; AMG8379
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Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
>14 μM
Compound: 15; AMG8379
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Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
| HEK293 | IC50 |
>14 μM
Compound: 15; AMG8379
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Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
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[PMID: 31012583] |
体外実験
AMG8379 is 100 to 1000-fold selective over other NaV family members, including NaV1.4 expressed in muscle and NaV1.5 expressed in heart, as well as TTX-resistant NaV channels in DRG neurons[1].
The IC50 for AMG8379 inhibition of C-fiber spiking based on the level of firing in NaV1.7 KO mice representing complete pharmacological block of the NaV1.7-component of this assay is calculated. In this manner, the IC50 for AMG8379 block is 47.0 ± 8.1 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 male mice[1]
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Dosage:30 or 100 mg/kg body weight
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Administration:Oral
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Result:Showed a dose-dependent reduction in overall nociceptive behavior.
化学情報
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CAS 番号 1642112-31-9
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分子量 543.93
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分子式 C25H16ClF2N3O5S
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SMILES
O=S(NC1=NOC=C1)(C2=CC(C=CC(N3C4=C(OC)C=C(C(F)=C4)C5=CC(Cl)=CC(F)=C5)=O)=C3C=C2)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
AMG8379 関連分類
HY-108425 関連分類
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