1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. Nav1.5-IN-1

Nav1.5-IN-1 is a selective Nav1.5 inhibitor with an IC50 of 1.38 μM. Nav1.5-IN-1 shows selectivity over other Nav subtypes. Nav1.5-IN-1 reduces cardiac conduction in isolated rat hearts.Nav1.5-IN-1 can be used for the research of arrhythmias.

For research use only. We do not sell to patients.

Nav1.5-IN-1

Nav1.5-IN-1 Chemical Structure

CAS No. : 899207-91-1

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Description

Nav1.5-IN-1 is a selective Nav1.5 inhibitor with an IC50 of 1.38 μM. Nav1.5-IN-1 shows selectivity over other Nav subtypes. Nav1.5-IN-1 reduces cardiac conduction in isolated rat hearts.Nav1.5-IN-1 can be used for the research of arrhythmias[1].

IC50 & Target[1]

Nav1.5

1.38 μM (IC50)

In Vitro

Nav1.5-IN-1 (KH2) potently inhibits wild-type human Nav1.5 in HEK293T cells with an IC50 of 1.38 μM and shows selectivity over other Nav subtypes[1].
Nav1.5-IN-1 (KH2) (500 ns) binds stably to the central cavity pocket of human Nav1.5 in MD simulations, with critical interactions involving residues C896, L931, and F1760[1].
Nav1.5-IN-1 (KH2) weakly inhibits hERG currents in HEK293T cells with an IC50 of 10.32 μM and does not significantly inhibit Kir2.1 at 20 μM[1].

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

In Vivo

Nav1.5-IN-1 (KH2) (35 mg/kg; i.p.; single dose) does not induce acute systemic or neurobehavioral toxicity in 8-week-old mice[1].

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

Animal Model: Mice (8-week-old)[1]
Dosage: 35 mg/kg
Administration: i.p.; single dose
Result: Showed no behavioral abnormalities in open-field (total distance traveled, time in central zone) or forced swim (immobility time) tests compared to controls.
Molecular Weight

642.21

Formula

C36H36ClN3O4S

CAS No.
SMILES

O=C(C1=CC2=C(S(=O)(C3=CC=CC=C3C(N2CC4=CC(Cl)=CC=C4)=O)=O)C=C1)NCCCN5CCC(CC5)CC6=CC=CC=C6

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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:
Nav1.5-IN-1
Cat. No.:
HY-181063
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