Kv1.5-IN-1
Kv1.5-IN-1 is a Kv1.5 channel inhibitor. Its target selectivity and pharmacodynamic effects were evaluated in an in vitro rat model. After the introduction of a methoxy group at the R5 position, Kv1.5-IN-1 showed inhibitory potency similar to that of the unsubstituted compound. Its IC50 value for hKv1.5 channels was 0.51 μM. Kv1.5-IN-1 exhibited a high degree of selectivity, nearly 2,600 times higher than compound Ik and 300 times higher than compound IId, indicating that it may be a safe inhibitor. Due to its good pharmacological behavior, Kv1.5-IN-1 deserves further pharmacodynamic and pharmacokinetic evaluation. These properties make Kv1.5-IN-1 a potential Kv1.5 channel inhibitor that may have application prospects in the treatment of related diseases.
For research use only. We do not sell to patients.
- CAS No.: 1469902-72-4
- Formula: C25H23ClN4O4S
- Molecular Weight:510.99
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
418.35 μM
Compound: IIIl
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Inhibition of human ERG channel expressed in CHO cells by whole cell patch clamp technique
Inhibition of human ERG channel expressed in CHO cells by whole cell patch clamp technique
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[PMID: 24071446] |
| HEK293 | IC50 |
0.51 μM
Compound: IIIl
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Inhibition of human Kv1.5 channel expressed in HEK293 cells by whole cell patch clamp technique
Inhibition of human Kv1.5 channel expressed in HEK293 cells by whole cell patch clamp technique
|
[PMID: 24071446] |
| Ventricular myocyte | IC50 |
52.6 μM
Compound: IIIl
|
Inhibition of sodium channel in guinea pig ventricular myocytes by whole cell patch clamp technique
Inhibition of sodium channel in guinea pig ventricular myocytes by whole cell patch clamp technique
|
[PMID: 24071446] |
Chemical Information
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CAS No. 1469902-72-4
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Molecular Weight 510.99
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Formula C25H23ClN4O4S
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SMILES
O=S(C1=CC=C(C)C=C1)(N/N=C/C2=CN(CC(NC3=CC=C(Cl)C=C3)=O)C4=C2C=C(OC)C=C4)=O
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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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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How to Select a Suitable Non-Mouse Animal Model
Selecting a suitable non-mouse animal model is a structured decision based on the research question, required anatomy or physiology, disease mechanism, endpoint feasibility, translational relevance, and ethical justification. Non-mouse models are preferred when mice cannot reproduce key human-relevant features, such as organ size, surgical anatomy, cardiovascular physiology, neuroanatomy, immune features, pharmacology, toxicology, or long-term clinical procedures. Candidate species may include rats, rabbits, guinea pigs, ferrets, zebrafish, pigs, sheep, goats, dogs, cats, horses, and non-human primates, but each species must be justified by its specific scientific advantage rather than convenience or tradition. Unresolved questions include how to quantify translational superiority across species, how to balance increased biological relevance against higher ethical burden, and when human-derived systems or new approach methodologies should replace animal use.
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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)