Delgocitinib is a novel and specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
Delgocitinib/迪高替尼 细胞实验
Cell Line
Concentration
Treated Time
Description
References
human T cells
8.9±3.6 nM (IC50)
3 days
inhibited IL-2-induced proliferation of T cells
Inflamm Res. 2015 Jan;64(1):41-51
normal human lung fibroblasts (NHLFs)
>10,000 nM (IC50)
3 days
no clear inhibitory effect
Inflamm Res. 2015 Jan;64(1):41-51
human mast cells
133±18 nM (IC50)
5 days
inhibited IL-4 and IgE-induced TNF-α production
Inflamm Res. 2015 Jan;64(1):41-51
human monocytes
277±146 nM (IC50)
16 h
inhibited GM-CSF-enhanced LPS-induced TNF-α production
Inflamm Res. 2015 Jan;64(1):41-51
human B cells
49±6 nM (IC50)
3 days
inhibited IL-21 and anti-CD40 antibody-induced B cell proliferation
Inflamm Res. 2015 Jan;64(1):41-51
Delgocitinib/迪高替尼 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Sclerodermatous GVHD mouse model
Topical administration (eyelids or back skin)
0.5% Delgocitinib ointment or eye drops
Twice daily for 21 consecutive days
To evaluate the efficacy of topical Delgocitinib in alleviating skin and ocular symptoms in GVHD mice. Results showed that Delgocitinib significantly increased the meibomian gland area, attenuated corneal epithelial damage, and reduced inflammation and pathological fibrosis.
搜索
