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.
Chemical Formula: C23H24ClN3O2
Exact Mass: 409.1557
Molecular Weight: 409.914
Elemental Analysis: C, 67.39; H, 5.90; Cl, 8.65; N, 10.25; O, 7.81
InChi Code: 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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
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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.
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