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].
|
|
References |
1. Irlapati NR, Deshmukh GK, Karche VP, Jachak SM, Sinha N, Palle VP, Kamboj RK. (2012)
Oxazole and isoxazole CRAC modulators. Patent number: WO2012056478. Assignee: Lupin Limited. Priority date: 31/10/2011. Publication date: 03/05/2012. |
2. Khedkar NR, Irlapatti NR, Dadke D, Kanoje V, Shaikh Z, Karche V, Shinde V, Deshmukh G, Patil A, Jachak S et al.. (2021)
Discovery of a Novel Potent and Selective Calcium Release-Activated Calcium Channel Inhibitor: 2,6-Difluoro-N-(2'-methyl-3'-(4-methyl-5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)-[1,1'-biphenyl]-4-yl)benzamide. Structure-Activity Relationship and Preclinical Characterization. J Med Chem, 64 (23): 17004-17030. [PMID:34843241] |