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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.).
| Molecular Weight | 304.73 |
| Formula | C18H9ClN2O |
| CAS Number | 23982-76-5 |
| Solubility (25°C) | DMSO: 0.5 mg/mL (warmed) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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