2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Sodium Channel Calcium Channel Potassium Channel
  4. ERG-IN-7

ERG-IN-7 is a Nav1.5, Cav1.2 and Kv11.1 inhibitor with IC50 values of 10.34 μM, 21.01 μM, and 16.385 μM for human Nav1.5, Cav1.2, and Kv11.1, respectively. ERG-IN-7 prolongs action potentials, reduces conduction velocity, and restores cardiac function. ERG-IN-7 can be used for the research of ventricular arrhythmia.

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

ERG-IN-7

ERG-IN-7 Chemical Structure

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ERG-IN-7 Related Antibodies

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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Description

ERG-IN-7 is a Nav1.5, Cav1.2 and Kv11.1 inhibitor with IC50 values of 10.34 μM, 21.01 μM, and 16.385 μM for human Nav1.5, Cav1.2, and Kv11.1, respectively. ERG-IN-7 prolongs action potentials, reduces conduction velocity, and restores cardiac function. ERG-IN-7 can be used for the research of ventricular arrhythmia[1].

IC50 & Target[1]

hNav1.5

10.34 μM (IC50)

Cav1.2

21.01 μM (IC50)

kv11.1

16.385 μM (IC50)

In Vitro

ERG-IN-7 (Compound 6-24) (0.3-100 μM) preferentially inhibits half-inactivated human Nav1.5 channels in HEK293 cells with an IC50 of 10.34 μM, showing noncooperative binding behavior[1].
ERG-IN-7 (1-100 μM) inhibits human Cav1.2 channels in HEK293 cells with an IC50 of 21.01 μM[1].
ERG-IN-7 (0.1-100 μM) weakly inhibits human Kv7.1, Kv4.3, and Kir2.1 channels in HEK293 cells (IC50 > 30 μM) and moderately inhibits human hERG channels with an IC50 of 16.385 μM[1].
ERG-IN-7 shows low cytotoxicity in H9c2 rat cardiomyocytes, with over 88% cell survival at concentrations up to 100 μM[1].

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

ERG-IN-7 Related Antibodies
Parmacokinetics
Species Dose Route C0 T1/2 CL Vdss AUC0-∞
Rat[1] 5 mg/kg i.v. 8108 ng/mL 1.70 h 26.8 mL/min/kg 1.75 L/kg 3136 ng·h/mL
In Vivo

ERG-IN-7 (Compound 6-24) (5 mg/kg; sublingual vein; single dose) exerts potent, long-lasting antiarrhythmic efficacy in BaCl2-induced arrhythmic rats, with a mean efficacy duration of 1693.17 s, while also normalizing cardiac structure, hemodynamic function, and repolarization intervals without significant QTc prolongation[1].

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

Animal Model: Sprague-Dawley (SD) (male, BaCl2-induced ventricular arrhythmia)[1]
Dosage: 5 mg/kg
Administration: sublingual vein; single dose
Result: Reduced mean onset time of recovery from arrhythmia to 11.33 s.
Extended mean duration of antiarrhythmic efficacy to 1693.17 s.
Maintained efficacy duration ≥20 min in all 6 treated rats.
Normalized postdose QT interval to 76.40 ms, matching the normal baseline of 75.82 ms.
Normalized postdose QTc interval to 0.206 ms, near the normal baseline of 0.212 ms.
Reduced heart rate to 424.17 bpm (P < 0.001 vs model group).
Normalized left ventricular ejection fraction (LVEF) to 87.05% (P < 0.001 vs model group).
Normalized fractional shortening (FS) to 45.84% (P < 0.001 vs model group).
Restored left ventricular internal dimension at end-diastole (LVIDd) to 0.507 cm (P < 0.05 vs model group, no significant difference vs normal baseline).
Restored left ventricular internal dimension at end-systole (LVIDs) to 0.282 cm (no significant difference vs normal baseline of 0.303 cm).
Restored cardiac output (CO) to near-baseline levels at 0.121 L/min.
Molecular Weight

378.42

Formula

C22H22N2O4
SMILES

O=C(N1CCC2=C3C1CC4=CC=CC=C4C3=C5C(OCO5)=C2)N6CCOCC6
Shipping

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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ERG-IN-7 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

ERG-IN-7Sodium ChannelCalcium ChannelPotassium ChannelNa channelsNa+ channelsCa2+ channelsCa channelsKcsAH9c2 rat cardiomyocyteshERG (Kv11.1)ventricular arrhythmiaKv4.3Nav1.5Kir2.1Cav1.2HEK293 cellshiPSC-CMsKv7.1Inhibitorinhibitorinhibit

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