Preferred Label : Zegocractin;
NCIt synonyms : CRAC Inhibitor CM4620; Orai Ca2 Channel Inhibitor CM4620; Orai1 Inhibitor CM4620; Calcium Release-activated Channel Inhibitor CM4620;
NCIt definition : A calcium (Ca2 ) release-activated channel (CRAC) inhibitor, with potential anti-inflammatory
and protective activities. Upon administration, zegocractin targets, binds to and
inhibits the calcium release-activated calcium channel protein 1 (Orai1), which forms
the pore of CRAC, and is expressed on both parenchymal cells and immune cells. This
prevents the transport of extracellular Ca2 into the cell and inhibits the subsequent
activation of Ca2 -mediated signaling and transcription of target genes. This may
prevent Ca2 entry-mediated cell death. It may also inhibit the proliferation of immune
cells and prevents the release of various inflammatory cytokines in immune cells,
such as interleukin-2 (IL-2) and tumor necrosis factor-alpha (TNF-a). This may lead
to a reduction of inflammatory responses in inflammatory-mediated diseases. CRACs,
specialized plasma membrane Ca2 ion channels composed of the plasma membrane based
Orai channels and the endoplasmic reticulum (ER) stromal interaction molecules (STIMs),
mediate store operated Ca2 entry (SOCE) and play a key role in calcium homeostasis.
CRACs are overactivated in a variety of cell types, especially certain immune cells
during inflammation, including T-lymphocytes, neutrophils and macrophages.;
UNII : 564AW1RR37;
CAS number : 1713240-67-5;
Molecule name : CM 4620; CM-4620;
NCI Metathesaurus CUI : CL971668;
Origin ID : C166417;
UMLS CUI : C5667197;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
