1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. 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.

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Kv1.5-IN-1 Chemical Structure

Kv1.5-IN-1 Chemical Structure

CAS No. : 1469902-72-4

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Description

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.

Cellular Effect
Cell Line Type Value Description References
CHO IC50
418.35 μM
Compound: IIIl
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
[PMID: 24071446]
HEK293 IC50
0.51 μM
Compound: IIIl
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]
Molecular Weight

510.99

Formula

C25H23ClN4O4S

CAS No.
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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Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Kv1.5-IN-1
Cat. No.:
HY-136805
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