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.
For research use only. We do not sell to patients.
- Formula: C22H27N3O4S
- Molecular Weight:429.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Adrenergic Receptor Isoforms
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Biological Activity
Description
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. Further protocols information, click here.
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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Formula 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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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.
Protocols
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)