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CAS No. : 2068119-11-7
MCE 国际站:S18-000003
产品活性:S18-000003 是一种有效,选择性和具有口服活性的维甲酸相关孤儿受体 (RORγt) 的抑制剂,在竞争性结合试验中,对 hRORγt 的 IC50 值小于 30 nM。S18-000003 对于 RORγt 的选择性高于其他 ROR 家族成员 (IC50>10 μM)。S18-000003 可用于研究银屑病,并且具有较低的胸腺畸变风险。
研究领域:Metabolic Enzyme/Protease | Vitamin D Related/Nuclear Receptor
作用靶点:ROR
In Vitro: S18-000003 inhibits human and mouse RORγt-dependent transactivation, with IC50s 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 IC50 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 IC50 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.
In Vivo: 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), CLtot (4.33 mL/min/kg) and Vdss in rats.
S18-000003 (1 mg/kg; p.o.) exhibits the oral bioavailability (54.5%), Cmax (185 ng/mL), AUC (2110 ng•h/mL) and Tmax (4 h) in rats.
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Metabolism/Protease Compound Library | Small Molecule Immuno-Oncology Compound Library | Orally Active Compound Library | Transcription Factor-Targeted Library | Nuclear Receptor Compound Library | Highly Selective Inhibitors Library | SR3335 | Methyl-3β-hydroxycholenate | Bevurogant | PF-06747711 | Zilovertamab | XY101 | RORγt inhibitor 2 | RORγt Inverse agonist 8 | RORγt agonist 3 | RORγt modulator 2 | SR0987 | AZD-0284 | RORγt Inverse agonist 6 | ARN-6039 | RORγ agonist 1 | RORγt/DHODH-IN-2 | SR1001 | 3-Oxo-5β-cholanoic acid | GNE-6468 | RORγt inverse agonist 29 | 7ß,27-Dihydroxycholesterol | Nobiletin | CD12681 | BMS-986251 | TAK-828F | RORγt inverse agonist 13 | RORγt Inverse agonist 3 | SHR168442 | GSK805 | SR1555
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