化合物GSK805 T7388

Product Introduction
Bioactivity


英文名: GSK805

描述: GSK805 是能够生物利用的、具有 CNS 穿透性的 RORγt 抑制剂。

细胞实验: CD4+CD62LhighCD25? naive CD4+ T cells were purified by FACS sorting following a MACS bead isolation of CD4+ cells. Naive CD4+ cells were activated with plate-bound anti-CD3 (2 μg/ml) and anti-CD28 (2 μg/ml). For Th17 cell differentiation, cultures were supplemented with IL-6 (20 ng/ml) plus TGF-β1 (1 ng/ml), and IL-23 (10 ng/ml) was added after 48 h. RORγt inhibitors or vehicle control DMSO was also included in the cultures. After 96 h, cells were collected for further experiments[1].

体外活性: GSK805 inhibits the expression of IL-17 (at 0.5 μM) in na?ve CD4+ T cells activated under Th17-cell-polarizing conditions and affects the broader RORγt-dependent gene network, inhibiting the development and pathogenic function of Th17 cells[1].

体内活性: GSK805 significantly reduces the severity of experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis, when given orally to the hosts at 10 mg/kg daily beginning at the time of disease induction[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (187.84 mM)
5% DMSO+95% Saline : 5 mg/mL (9.39 mM, suspension)


关键字: GSK 805 | immunity | RAR-related orphan receptor | Inhibitor | inhibit | ROR | oral | CNS penetrant | Th17 cell | GSK-805 | GSK805

相关产品: S18-000003 | TMP780 | Cintirorgon | TAK-828F | ML 209 | Cedirogant | SR1001 | SR1078 | Cabozantinib hydrochloride | RORγt inverse agonist 31

相关库: Transcription Factor-Targeted Compound Library | Bioactive Compounds Library Max | CNS-Penetrant Compound Library | Inhibitor Library | Kinase Inhibitor Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Orally Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途