Uses
7-?Chloro-?1,?5-?dihydro-?5-?[2-?(1-?methylethyl)?phenyl]?-4,?1-benzothiazepin-?2(3H)?-?one can be used to study the physiological roles of the mitochondrial sodium /calcium exchanger related to neurodegeneration.
Biological Activity
ITH12575 is apotent and selective inhibitor of mitochondrial Na+/Ca2+ exchanger mNCX with neuroprotective activity. It was shown to reduce Ca2+ efflux from the mitochondria to the cytosol with an EC50 value of 690 nM and was shown to protect against Ca2+ overload and mitigated the neuronal damage in a model of oxidative stress. at higher concentrations ITH12575 also reduced Ca2+ influx through CALHM1, a Ca2+ channel th at plays a key role in the neuronal electrical activity.
