FR-168888 free base
FR-168888 free base 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 free base is widely applicable to studies related to reperfusion-induced ventricular arrhythmias.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 168620-45-9
- Formel: C13H14N4O2
- Molecular Weight:258.28
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
In Vitro
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.
-
Animal Model:Sprague-Dawley (male, 250-400 g, myocardial ischemia-reperfusion injury model)[1]
-
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)
-
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
-
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
-
CAS. Nr. 168620-45-9
-
Molecular Weight 258.28
-
Formel C13H14N4O2
-
SMILES
O=C(NC(=N)N)C=1C=C(C=C(C1)CO)N2C=CC=C2
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Keywords
- FR-168888
- 168620-45-9
- FR168888
- FR 168888
- Na+/H+ Exchanger (NHE)
- Sodium/hydrogen Exchanger
- Sodium-hydrogen Exchanger
- Na+/Ca2+ exchanger
- Na+/H+ exchanger
- rat cardiac sarcolemmal vesicles
- reperfusion-induced ventricular fibrillation
- anesthetized rats
- reperfusion-induced ventricular arrhythmias
- rat thymic lymphocytes
- Inhibitor
- inhibitor
- inhibit