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.
For research use only. We do not sell to patients.
- CAS No.: 168620-45-9
- Formula: C13H14N4O2
- Molecular Weight:258.28
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
FR-168888 free base 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.
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. 168620-45-9
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Molecular Weight 258.28
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Formula C13H14N4O2
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SMILES
O=C(NC(=N)N)C=1C=C(C=C(C1)CO)N2C=CC=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FR-168888 free base Related Classifications
HY-187612 Related Classifications
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