1,6-Diazaspiro[3.4]octane, 3-methyl-1-(phenylmethyl)-, ethanedioate (2:1), (3S,4R) Used For Delgocitinib CAS 2230683-29-9

Thera. Category:Atopic dermatitis

Cas No.:2230683-29-9

Synonyms:1,6-Diazaspiro[3.4]octane, 3-methyl-1-(phenylmethyl)-, ethanedioate (2:1), (3S,4R)-;Delgocitinib  intermediate;JTE-052 Intermediates;

Molecular Formula: C16H22N2O4

Molecular Weight:306.36

Purity: ≥98%

Packing: Export worthy packing

Material Safety Data Sheet: Available on request

Usage : Delgocitinib as known as  JTE-052,which is a novel and specific inhibitor of JAK (IC50s: 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively) .Delgocitinib inhibits the phosphorylation of Stat proteins induced by IL-2, IL-6, IL-23, GM-CSF, and IFN-α (IC50: 40±9, 33±14, 84±11, 304±22 and 18±3 nM, respectively), in these cell-based cytokine signaling assays and it also inhibits IL-2-induced proliferation of T cells in a concentration-dependent manner (IC50: 8.9±3.6 nM). Its potency is similar to that of tofacitinib (IC50:16 nM). Delgocitinib effectively inhibits all of the JAK subtypes ( IC50: 2.8±0.6, 2.6±0.2, 13±0 and 58±9 nM for JAK1, JAK2, JAK3 and Tyk2, respectively), in the enzymatic assays. Lineweaver-Burk plots display that the inhibition mode of Delgocitinib toward all JAKs is competitive with ATP (Ki: 2.1±0.3, 1.7±0.0, 5.5±0.3 and 14±1 nM for JAK1, JAK2, JAK3 and Tyk2, respectively)