1. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  2. Potassium Channel Sodium Channel Adrenergic Receptor
  3. 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.

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hERG-IN-3

hERG-IN-3 Chemical Structure

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Description

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[1].

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

hERG-IN-3 (1 mg/kg, p.o., single dose) significantly improves muscle rigidity symptoms in rat myotonia model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Myotonia model established in adult Wistar rats (350/500 g)[1]
Dosage: 1 mg/kg
Administration: Oral administration (p.o.), single dose
Result: The reduction of the time of righting reflex in vivo in the rat model of myotonia was observed.
Molecular Weight

429.53

Formula

C22H27N3O4S

SMILES

OC(COC1=CC=CC(O)=C1)CN2CCC(N(C3=NC4=CC=C(O)C=C4S3)C)CC2

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Product Name:
hERG-IN-3
Cat. No.:
HY-175289
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