AL 082D06

AL082D06, also known as D-06, is a nonsteroidal glucocorticoid receptor antagonist. AL082D06 binds specifically to GR with no measurable binding affinity to the progesterone receptor. AL082D06 binds with nanomolar affinity to the GR and has no detectable binding affinity for the highly related receptors for mineralocorticoids, androgens, estrogens, and progestins. AL082D06 inhibits glucocorticoid-mediated transcriptional regulation. AL082D06 binds competitively with steroids, likely occupying a similar site within the ligand-binding domain.

Product information

CAS Number: 256925-03-8

Molecular Weight: 409.91

Formula: C23H24ClN3O2

Synonym:

D-06

AL082D06

AL-082D06

AL 082D06

Chemical Name: 4,4'-((2-chloro-5-nitrophenyl)methylene)bis(N,N-dimethylaniline)

Smiles: CN(C)C1C=CC(=CC=1)C(C1=CC(=CC=C1Cl)[N+]([O-])=O)C1C=CC(=CC=1)N(C)C

InChiKey: IPICUXHYPAMJNC-UHFFFAOYSA-N

InChi: InChI=1S/C23H24ClN3O2/c1-25(2)18-9-5-16(6-10-18)23(17-7-11-19(12-8-17)26(3)4)21-15-20(27(28)29)13-14-22(21)24/h5-15,23H,1-4H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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.

References:

1. Quiroz JA, Singh J, Gould TD, Denicoff KD, Zarate CA, Manji HK. Emerging experimental therapeutics for bipolar disorder: clues from the molecular pathophysiology. Mol Psychiatry. 2004 Aug;9(8):756-76. Review. PubMed PMID: 15136795.
2. Miner JN, Tyree C, Hu J, Berger E, Marschke K, Nakane M, Coghlan MJ, Clemm D, Lane B, Rosen J. A nonsteroidal glucocorticoid receptor antagonist. Mol Endocrinol. 2003 Jan;17(1):117-27. PubMed PMID: 12511611.

Products are for research use only. Not for human use.