Synonyms: example 48 [WO2012056478]
Compound class:
Synthetic organic
Comment: This compound is reported as an inhibitor of calcium release-activated calcium (CRAC) channel activity [2]. CRAC channels contain Orai1 (the pore-forming subunit) and stromal interaction molecule 1 (STIM1, which senses Ca2+ levels in the endoplasmic reticulum), and they mediate influx of Ca2+ ions into T cells in response to antigen engagement. CRAC function inhibitors have anti-inflammatory potential via blocking NFAT-mediated T cell activation. The chemical structure was claimed in Lupin Limited's 2012 patent WO2012056478A1 [1].
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Bioactivity Comments |
Compound 36 inhibits antigen-activated IL-2 and TNFα release from T cells, and is active in in vivo rheumatoid arthritis models [2]. Inhibits CRAC-channel mediated store-operated calcium entry (SOCE) with an in vitro IC50 of 11 nM [2]. |
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