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化驗
≥97% (HPLC)
形狀
lyophilized powder
顏色
white to off-white
運輸包裝
wet ice
儲存溫度
−20°C
SMILES 字串
FC(F)(C(O)=O)F.NC(NCCC[C@@H](C(N1CCC[C@H]1C(N)=O)=O)NC(C2=C(O)C3=CC=CC=C3C=C2)=O)=N
InChI
1S/C22H28N6O4/c23-19(30)17-8-4-12-28(17)21(32)16(7-3-11-26-22(24)25)27-20(31)15-10-9-13-5-1-2-6-14(13)18(15)29/h1-2,5-6,9-10,16-17,29H,3-4,7-8,11-12H2,(H2,23,30)(H,27,31)(H4,24,25,26)/t16-,17-/m0/s1
InChI 密鑰
SKYWIMYOGAWOMB-IRXDYDNUSA-N
生化/生理作用
APC366 is a selective inhibitor of mast cell tryptase, which is involved with allergenic response. It thereby also inhibits protease-activated receptor PAR2, a G-protein-coupled receptor that is activated by mast cell tryptase. Tryptase has been proposed to be involved in fibrosis, joint inflammation and also in promoting breast cancer angiogenesis, all of which APC366 inhibited.
International archives of allergy and immunology, 177(3), 199-206 (2018-07-19)
Mast cells are key immune effector cells which release chemokines, proteases, and other inflammatory mediators upon activation by immunological stimuli. The aim of this study was to investigate the effects of co-releasing proteases on the kinetics of release of the
Oncology letters, 16(2), 1513-1520 (2018-07-17)
Mast cells have been demonstrated to accumulate around and within solid tumors of numerous types, and express a number of pro-angiogenic compounds, including tryptase. They may serve an early role in angiogenesis within developing tumors. In the present study, the
Arthritis research & therapy, 19(1), 124-124 (2017-06-08)
Increasing evidences indicate that an unbalance between tryptases and their endogenous inhibitors, leading to an increased proteolytic activity, is implicated in the pathophysiology of rheumatoid arthritis. The aim of the present study was to evaluate the impact of tryptase inhibition
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