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hERG-IN-3 is an orally active hERG inhibitor with an IC50 of 44.5 nM. It has a Ki value of 14 nM for the β2-adrenergic receptor. hERG-IN-3 exhibits skeletal muscle Nav1.4 sodium channel blocking activity with an IC50 of 4.4 μM, which is three times higher than that for hNav1.5. In animal models, hERG-IN-3 demonstrates potent antimyotonic activity and can be utilized in the study of congenital myotonia.
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| 10 mg | Inquiry | Inquiry | Inquiry | |
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| Description | hERG-IN-3 is an orally active hERG inhibitor with an IC50 of 44.5 nM. It has a Ki value of 14 nM for the β2-adrenergic receptor. hERG-IN-3 exhibits skeletal muscle Nav1.4 sodium channel blocking activity with an IC50 of 4.4 μM, which is three times higher than that for hNav1.5. In animal models, hERG-IN-3 demonstrates potent antimyotonic activity and can be utilized in the study of congenital myotonia. |
| Targets&IC50 | α1A-adrenoceptor:270 nM |
| In vitro | hERG-IN-3 exhibits affinity for the α1A and β2 receptors with K i values of 270 nM and 14 nM, respectively. It also has a relaxing effect on K + depolarized guinea pig ileal longitudinal smooth muscle, with an IC 50 of 0.83 μM. |
| In vivo | Administered orally at a dose of 1 mg/kg, hERG-IN-3 significantly alleviates muscle stiffness symptoms in a rat model of myotonia. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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