FR168888
FR-168888 is a Na+/H+ exchanger (NHE) inhibitor (Ki=6.4 nM) with weak inhibitory activity against Na+/Ca2+ exchanger and no cardioprotective effects. FR-168888 is widely applicable to studies related to reperfusion-induced ventricular arrhythmias.
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- CAS No.: 168620-46-0
- Formule: C14H18N4O5S
- Masse moléculaire:354.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
In Vitro
FR-168888 potently inhibits Na+/H+ exchange in rat thymic lymphocytes and weakly inhibits Na+/Ca2+ exchange in rat cardiac sarcolemmal vesicles[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 250-400 g, myocardial ischemia-reperfusion injury model)[1]
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Dosage:0.3 mg/kg (pre-ischemic); 0.3 mg/kg (post-ischemic); 1 mg/kg (post-ischemic); 3 mg/kg (post-ischemic); 10 mg/kg (post-ischemic); 3 mg/kg (1 min post-occlusion); 3 mg/kg (immediately before reperfusion)
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Administration:i.v.; 5 min before coronary occlusion; i.v.; 3 min after coronary occlusion; i.v.; 1 min after coronary occlusion; i.v.; immediately before reperfusion
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Result:Reduced reperfusion-induced ventricular fibrillation (VF) incidence to 10% and mortality to 0% (pre-ischemic 0.3 mg/kg).
Reduced VF incidence to 70% and mortality to 50% (post-ischemic 0.3 or 1 mg/kg).
Reduced VF incidence to 60% and mortality to 30% (post-ischemic 3 or 10 mg/kg).
Increased mean blood pressure by 11 mmHg (3 mg/kg) and 10 mmHg (10 mg/kg) 1 minute after administration, and by 9 mmHg (3 mg/kg) and 12 mmHg (10 mg/kg) 2 minutes after administration (post-ischemic 3 or 10 mg/kg).
Reduced mortality to 30% across all post-ischemic 3 mg/kg administration time points.
Reduced VF incidence to 60% (1 min and 3 min post-occlusion) and 30% (immediately before reperfusion) (time-dependent post-ischemic 3 mg/kg).
Chemical Information
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CAS No. 168620-46-0
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Masse moléculaire 354.38
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Formule C14H18N4O5S
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SMILES
O=C(NC(N)=N)C1=CC(N2C=CC=C2)=CC(CO)=C1.CS(=O)(O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FR168888 Related Classifications
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