2016年6月13日星期一

AL 082D06(D-06)|CAS 256925-03-8

AL 082D06(D-06)|CAS 256925-03-8

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).

Product Name: AL 082D06(D-06)|Cat No: DC9677|Cas: 256925-03-8|Molecule Formular: C23H24ClN3O2|Molecule Weight: 409.91|Other names: AL 082D06(D-06)

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.

For research only, not for human use.


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