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.
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- 화학식: C22H22N2O4
- 분자량:378.42
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Help & FAQs
All Calcium Channel Isoforms
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Biological Activity
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hNav1.5 10.34 μM (IC50) |
Cav1.2 21.01 μM (IC50) |
kv11.1 16.385 μM (IC50) |
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.
| 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) (male, BaCl2-induced ventricular arrhythmia)[1]
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Dosage:5 mg/kg
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Administration:sublingual vein; single dose
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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.
Chemical Information
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분자량 378.42
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화학식 C22H22N2O4
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SMILES
O=C(N1CCC2=C3C1CC4=CC=CC=C4C3=C5C(OCO5)=C2)N6CCOCC6
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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