hERG-IN-3
hERG-IN-3 is an orally active hERG blocker with an IC50 of 44.5 nM. hERG-IN-3 exhibits a Ki for β2-adrenergic receptor of 14 nM. hERG-IN-3 exhibits the skeletal muscle Nav1.4 and sodium channel-blocking activities (IC50 = 4.4 μM, 3-fold increasement than hNav1.5). hERG-IN-3 displays a potent antimyotonic activity in an animal model. hERG-IN-3 can be used for the study of Myotonia Congenita.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C22H27N3O4S
- Molecular Weight:429.53
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Beta-2 adrenergic receptor 14 nM (IC50) |
α1A-adrenergic receptor 270 nM (IC50) |
Nav1.4 4.4 μM (IC50) |
Nav1.5 12 μM (IC50) |
In Vitro
hERG-IN-3 exhibits affinity on α1A and β2 receptors with Kis of 270 and 14 nM[1].
hERG-IN-3 exhibits relaxant activity of the tested compounds on K+-depolarized guinea pig longitudinal ileum smooth muscle with an IC50 of 0.83 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Myotonia model established in adult Wistar rats (350/500 g)[1]
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Dosage:1 mg/kg
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Administration:Oral administration (p.o.), single dose
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Result:Observed the reduction of the time of righting reflex in vivo in the rat model of myotonia.
Chemical Information
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Molecular Weight 429.53
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Formel C22H27N3O4S
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SMILES
OC(COC1=CC=CC(O)=C1)CN2CCC(N(C3=NC4=CC=C(O)C=C4S3)C)CC2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
hERG-IN-3 Related Classifications
HY-175289 Related Classifications
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