10-Cl-BBQ
规格
| Cas Number | 23982-76-5 |
| 规格或纯度 | ≥97%(HPLC) |
| 纯度 | ≥97%(HPLC) |
| 包装 | 100mg 或 50mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | 溶于DMSO, 最高浓度 (mg/mL): 0.3, 最高浓度(mM): 1 温和加热 |
| 简短描述 | 强效的芳烃受体（AhR）激动剂 |
| 英文简短描述 | Potent aryl hydrocarbon receptor (AhR) agonist |
| 储存温度 | 2-8°C储存 |
| 运输条件 | 冰袋运输 |
| 生化和生理学机理 | 潜在的芳基碳氢化合物受体（AhR）激动剂，被发现为筛选成功（IC50 = 2.6 nM）。直接结合CD4 + T细胞以诱导依赖AhR的Treg。抑制NOD小鼠的IL-17产生并预防胰岛炎。体内半衰期约2小时，口服可生物利用。10-Cl-BBQ is an orally bioavailable, non-toxic benzimidazoisoquinoline derivative that acts as an aryl hydrocarbon receptor (AhR) agonist via directly binding to AhR (IC50 = 2.6 nM in a competitive binding assay) and induces its nuclear translocation. 10-Cl-BBQ is shown to increase CD4+ T-cells that co-express CD25, CTLA-4 and ICOS, as well as several other genes associated with regulatory T cell (Treg) function in a graft versus host response model (GVH, C57BI/6 T cells injected into B6D2F1 host mice). 10-Cl-BBQ displays good pharmacokinetic profile in mice (t1/2 = 2 h, Cmax = 21.5 μg/L, 10 mg/kg, i.p.). Also shown to prevent insulitis in a NOD T1D mouse model which is independent of Fox3 + Tregs (60 mg/kg, p.o, q.o.d.). |