Details
Stereochemistry | ACHIRAL |
Molecular Formula | C12H17N3O3S.CH4O3S |
Molecular Weight | 379.452 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(O)(=O)=O.CC(C)C1=C(C=C(C=C1)C(=O)NC(N)=N)S(C)(=O)=O
InChI
InChIKey=FNDLQABGYJQJPH-UHFFFAOYSA-N
InChI=1S/C12H17N3O3S.CH4O3S/c1-7(2)9-5-4-8(11(16)15-12(13)14)6-10(9)19(3,17)18;1-5(2,3)4/h4-7H,1-3H3,(H4,13,14,15,16);1H3,(H,2,3,4)
Cariporide is a selective sodium-hydrogen antiporter inhibitor patented by a pharmaceutical company Hoechst A.-G. for treatment myocardial ischemia-reperfusion injury. The sodium-hydrogen exchanger is an important player in the pathophysiology of myocardial ischemia-reperfusion injury. The accumulation of hydrogen ions in the myocyte cytosol; during ischemia creates a proton gradient that promotes the efflux of hydrogen ions in exchange for the influx of sodium ions. This sodium buildup can secondary activates the sodium-calcium exchanger to operate in the reverse mode, resulting in a net calcium accumulation in myocyte cytosol, which leads to dysfunction and cell death. By inhibiting sodium-hydrogen exchange, Cariporide can prevent the accumulation of calcium in the cytosol, therefore reduce the infarct size. In clinical trials, Cariporide shows a statistically significant decline in myocardial infarction but increases mortality. Due to the increase in mortality, cariporide did not pass clinical trials.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2781 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24195657 |
65.0 nM [IC50] | ||
Target ID: CHEMBL3133 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11563929 |
62000.0 nM [IC50] |
PubMed
Title | Date | PubMed |
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Antiarrhythmic effects of HOE642, a novel Na(+)-H+ exchange inhibitor, on ventricular arrhythmias in animal hearts. | 1996 Dec 19 |
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[Protective effect of Na(+)-H+ exchanger inhibitor cariporide on the injury of vascular endothelial function induced by hypercholesterolemia]. | 2002 Feb 28 |
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An overview of inhibitors of Na(+)/H(+) exchanger. | 2003 Jun |
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Coordinated role of voltage-gated sodium channels and the Na+/H+ exchanger in sustaining microglial activation during inflammation. | 2013 Dec 1 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/30849956
120 mg 3 times a day
Route of Administration:
Oral
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NCI_THESAURUS |
C47793
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C81346
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178019
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m3110
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159138-81-5
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CHEMBL436559
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DTXSID3047344
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PP-60
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DBSALT002017
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ACTIVE MOIETY
SUBSTANCE RECORD