AL 082D06(D-06)

  Cat. No.:  DC9677   Featured
Chemical Structure
256925-03-8
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Field of application
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).
Cas No.: 256925-03-8
Chemical Name: AL 082D06
Synonyms: AL 082D06;4-[(2-chloro-5-nitrophenyl)-[4-(dimethylamino)phenyl]methyl]-N,N-dimethylaniline;D 06;AL-082D06;D-06;4,4'-[(2-Chloro-5-nitrophenyl)methylene]bis[N,N-dimethylbenzenamine]
SMILES: O=[N+](C1=CC=C(Cl)C(C(C2=CC=C(N(C)C)C=C2)C3=CC=C(N(C)C)C=C3)=C1)[O-]
Formula: C23H24N3O2Cl
M.Wt: 409.909
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: AL 082D06 is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.
In Vitro: AL 082D06 (D06) binds specifically to GR with nanomolar affinity. Addition of AL 082D06 causes a dose-dependent decrease in transcriptional activation from the MMTV:Luc reporter stimulated with half-maximal DEX concentrations. AL 082D06 acts to antagonize reporter activity using several glucocorticoid-responsive promoter- reporter systems including the 3-kb tyrosine amino transferase (TAT) promoter and less complex promoters comprised of isolated glucocorticoid response element (GRE) sequences. AL 082D06 competes with 3H-Dex for baculovirus-expressed GR with nanomolar affinity. Other intracellular receptors (AR, ER, PR, and MR) have no affinity for AL 082D06 in a similarly structured binding assay with the appropriate receptor and tritiated ligand (>2500 nM). AL 082D06 has no activation efficacy on the progesterone, androgen, mineralocorticoid, retinoid, glucocorticoid, or estrogen receptors. AL 082D06 is very efficacious at antagonizing GR activity but exhibits much weaker efficacy when tested against the other steroid receptors in contrast to the reference antagonists used as controls[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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