2068119-11-7
基本信息
物理化學(xué)性質(zhì)
常見問題列表
RORγt <30 nM (IC 50 ) |
S18-000003 inhibits human and mouse RORγt-dependent transactivation, with IC
50
s of 0.029 and 0.34 μM respectively in cell-based GAL4 promoter reporter assays.
S18-000003 (0.003-0.3 μM; 7 d) dose-dependently inhibits Th17 cell differentiation from human naive CD4
+
T cells, with an IC
50
of 0.024 μM.
S18-000003 (0.1-3 μM; 4 d) inhibits the differentiation of mouse Th17 cells from splenic naive CD4
+
T cells, with an IC
50
of 0.20 μM.
S18-000003 (0.03-1 μM; 3 d) reduces the IL-17 production in human PBMCs in a dose-dependent manner, and does not inhibit either the production of other cytokines (IL-2, IL-4, IL-10 and IFN-g) or cell proliferation.
S18-000003 (0.1-3 μM; 3 d) reduces IL-17 and IL-22 production in PBMCs from psoriatic mice in a dose-dependent manner.
S18-000003 (30-100 mg/kg; p.o.) inhibits IL-17 production in the skin of IL-23-treated mice in a dose-dependent manner.
S18-000003 (0.1-8%; 100mL; topically administration once daily for 14 days) ameliorates psoriasis-like lesions in TPA-induced K14.Stat3C transgenic mice, and has little impact on the thymus.
S18-000003 (0.5 mg/kg; i.v.) exhibits the half-life (3.2 h), AUC (1930 ng?h/mL), CL
tot
(4.33 mL/min/kg) and Vd
ss
in rats.
S18-000003 (1 mg/kg; p.o.) exhibits the oral bioavailability (54.5%), C
max
(185 ng/mL), AUC (2110 ng?h/mL) and T
max
(4 h) in rats.