Details
Stereochemistry | ACHIRAL |
Molecular Formula | C12H17N3O3S |
Molecular Weight | 283.347 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)C1=C(C=C(C=C1)C(=O)NC(N)=N)S(C)(=O)=O
InChI
InChIKey=IWXNYAIICFKCTM-UHFFFAOYSA-N
InChI=1S/C12H17N3O3S/c1-7(2)9-5-4-8(11(16)15-12(13)14)6-10(9)19(3,17)18/h4-7H,1-3H3,(H4,13,14,15,16)
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 |
---|---|---|---|
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] |
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
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NCI_THESAURUS |
C47793
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
m3110
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | Merck Index | ||
|
100000084614
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | |||
|
7395
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | |||
|
SUB06630MIG
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | |||
|
C76028
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | |||
|
DB06468
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | |||
|
7E3392891K
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | |||
|
C093373
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | |||
|
151172
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | |||
|
Cariporide
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | |||
|
CHEMBL436559
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | |||
|
DTXSID8047345
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY | |||
|
159138-80-4
Created by
admin on Fri Dec 15 16:21:17 GMT 2023 , Edited by admin on Fri Dec 15 16:21:17 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
SALT/SOLVATE (PARENT)