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FR183998 free base

Catalog No. T11319   CAS 239440-20-1

FR183998 free base is an inhibitor of Na+/Ca2+ Exchanger.

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FR183998 free base Chemical Structure
FR183998 free base, CAS 239440-20-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 349.00
5 mg In stock $ 690.00
10 mg In stock $ 992.00
25 mg In stock $ 1,470.00
50 mg In stock $ 1,980.00
100 mg In stock $ 2,680.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description FR183998 free base is an inhibitor of Na+/Ca2+ Exchanger.
Targets&IC50 Na+, H+ exchange (human platelet):3.1 nM , Na+, H+ exchange (rat lymphocytes):0.3 nM , Na+, H+ exchange (rat platelet):6.5 nM
In vitro FR183998 free base has potent inhibitory effects on Na+/H+ exchanger in rat lymphocytes, rat platelets, and human platelets with IC50s of 0.3 nM, 6.5 nM, and 3.1 nM, respectively[1].
In vivo Administered intravenously at 1 mg/kg, FR183998 free base diminishes the serum elevation of alanine transaminase, aspartate transaminase, and lactate dehydrogenase caused by hepatic ischemia/reperfusion (I/R), while also preventing hepatic necrosis, apoptosis, and neutrophil infiltration. It inhibits the I/R-triggered activation of NF-κB, downregulates iNOS induction, and curbs nitric oxide production, in addition to reducing the liver's iNOS gene antisense transcript expression in hepatic I/R rats. At dosages of 0.1 and 1.0 mg/kg via intravenous injection, FR183998 free base does not alter hemodynamic parameters, mean blood pressure, or heart rate in conscious rats. Both pre- and post-treatment with FR183998 free base, in doses ranging from 0.01 to 0.10 mg/kg intravenously, dose-dependently mitigates reperfusion-induced ventricular fibrillation and mortality in anesthetized rats, showing ED50 values against ventricular fibrillation of 0.015 mg/kg and 0.070 mg/kg, respectively. Moreover, it significantly reduces myocardial infarct sizes and suppresses arrhythmias in anesthetized rats.
Molecular Weight 428.34
Formula C17H19Cl2N5O2S
CAS No. 239440-20-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 200 mg/mL (466.9 mM), Sonication is recommended.

TargetMolReferences and Literature

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. 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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library ReFRAME Related Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library

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Benzamil CGP37157 KB-R7943 mesylate SN 6 Terfenadine PPADS tetrasodium SM-6586 SEA0400

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Keywords

FR183998 free base 239440-20-1 Membrane transporter/Ion channel Na+/Ca2+ Exchanger FR-183998 FR 183998 FR-183998 free base FR183998 inhibitor inhibit

 

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