2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
AL 082D06(D-06) is the first selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM, exhibits excellent selectivity against AR, PR, MR and ER(Ki > 10 uM).The antagonists NET, DO6 and UDCA, as well as the dissociated GC ligand CpdA (14%) resulted in little to no increase in S226 phosphorylation. The antagonists NET, DO6 and UDCA (13%, 8% and 21%), as well as the dissociated GC ligand CpdA (24%) resulted in little increase in S211 phosphorylation. D06 competes with 3H-Dex for baculovirus-expressed GR with nanomolar affinity. Other intracellular receptors (AR, ER, PR, and MR) have no affinity for D06 in a similarly structured binding assay with the appropriate receptor and tritiated ligand (>2500 nM). D06 can antagonize steroid-mediated induction of glutamine synthetase RNA in MG63 cells (data not shown) and TAT enzyme in human skin fibroblasts.
