FR183998 free base
Based on 1 Customer Validation
FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.00%
- CAS. Nr.: 239440-20-1
- Formel: C17H19Cl2N5O2S
- Molecular Weight:428.34
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
IC50: 0.3 nM (Na+/H+-exchange, Rat lymphocytes), 3.1 nM (Na+/H+-exchange, Human platelet), 6.5 nM (Na+/H+-exchange, Rat platelet)[1]
FR183998 free base is a Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 6.5 nM and 3.1 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively[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.
Chemical Information
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CAS. Nr. 239440-20-1
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Appearance Solid
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Molecular Weight 428.34
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Formel C17H19Cl2N5O2S
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Color White to off-white
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SMILES
O=C(C1=CC(C2=C(Cl)SC(Cl)=C2)=CC(C(NCCN(C)C)=O)=C1)NC(N)=N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 250 mg/mL (583.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
Intracellular pH of rats lymphocytes is measured at 37°C with a spectrofluorometer by using the ratio of the emission (530 nm) obtained at 490- and 440-nm excitation wavelengths. After addition of 10 μL of the BCECF- and acid-loaded cells to 460 μL of Na-free buffer with 5 μL of DMSO or FR183998, 25 μL of 2.0 M NaCl (final 100 mM) is applied to start the reaction. The pHi change of cells is measured for >2 min. The initial increase in pHi in response to the added NaCl is taken as an estimate of Na+/H+-exchange activity, and the inhibitory effect of the drug is evaluated as IC50 value. The BCECF fluorescence signals are calibrated by titration with stepwise addition of small volumes of 1 M MES after permeabilization of the cells with 0.5% Triton X-100[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male Sprague-Dawley rats age 9-10 weeks are anesthetized with sodium pentobarbital (50 mg/kg, i.p.), intubated, and ventilated with room air at a stroke volume of 4.5 mL with a frequency of 50 strokes/min. Saline or FR183998 is injected into the left femoral vein (bolus i.v.) 5 min before occlusion. Thoracotomy for coronary artery ligation is performed at the left side of the thorax above the heart, and the origin of the left anterior descending coronary artery is occluded by applying negative tension by aspiration through polyethylene tubing connected to the vacuum system, which can achieve regional ischemia. Successful occlusion is confirmed by ischemia-induced alteration of electrocardiogram (ECG). After 5-min ischemia, reperfusion is performed, and the incidence of ventricular tachycardia (VT) and ventricular fibrillation (VF) of >5 s is observed intermittently over a 5-min period of reperfusion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Ohara F, et al. Preischemic and postischemic treatment with a new Na+/H+-exchange inhibitor, FR183998, shows cardioprotective effects in rats with cardiac ischemia and reperfusion. J Cardiovasc Pharmacol. 1999 Dec;34(6):848-56. [Content Brief]
[2]. Ishizaki M, et al. Protective effect of FR183998, a Na+/H+ exchanger inhibitor, and its inhibition of iNOS induction in hepatic ischemia-reperfusion injury in rats. Shock. 2008 Sep;30(3):311-7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3346 mL | 11.6730 mL | 23.3459 mL | 58.3649 mL |
| 5 mM | 0.4669 mL | 2.3346 mL | 4.6692 mL | 11.6730 mL | |
| 10 mM | 0.2335 mL | 1.1673 mL | 2.3346 mL | 5.8365 mL | |
| 15 mM | 0.1556 mL | 0.7782 mL | 1.5564 mL | 3.8910 mL | |
| 20 mM | 0.1167 mL | 0.5836 mL | 1.1673 mL | 2.9182 mL | |
| 25 mM | 0.0934 mL | 0.4669 mL | 0.9338 mL | 2.3346 mL | |
| 30 mM | 0.0778 mL | 0.3891 mL | 0.7782 mL | 1.9455 mL | |
| 40 mM | 0.0584 mL | 0.2918 mL | 0.5836 mL | 1.4591 mL | |
| 50 mM | 0.0467 mL | 0.2335 mL | 0.4669 mL | 1.1673 mL | |
| 60 mM | 0.0389 mL | 0.1945 mL | 0.3891 mL | 0.9727 mL | |
| 80 mM | 0.0292 mL | 0.1459 mL | 0.2918 mL | 0.7296 mL | |
| 100 mM | 0.0233 mL | 0.1167 mL | 0.2335 mL | 0.5836 mL |