MedKoo Cat#: 522627 | Name: AL082D06
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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 Structure

AL082D06
AL082D06
CAS#256925-03-8

Theoretical Analysis

MedKoo Cat#: 522627

Name: AL082D06

CAS#: 256925-03-8

Chemical Formula: C23H24ClN3O2

Exact Mass: 409.1557

Molecular Weight: 409.91

Elemental Analysis: C, 67.39; H, 5.90; Cl, 8.65; N, 10.25; O, 7.81

Price and Availability

Size Price Availability Quantity
25mg USD 185.00 Ready to ship
50mg USD 285.00 Ready to ship
100mg USD 450.00 Ready to ship
200mg USD 750.00 Ready to ship
500mg USD 1,650.00 Ready to ship
1g USD 2,650.00 Ready to ship
2g USD 4,650.00 Ready to ship
5g USD 6,450.00 2 Weeks
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Related CAS #
No Data
Synonym
AL082D06; AL-082D06; AL 082D06; D-06.
IUPAC/Chemical Name
4,4'-((2-chloro-5-nitrophenyl)methylene)bis(N,N-dimethylaniline)
InChi Key
IPICUXHYPAMJNC-UHFFFAOYSA-N
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
SMILES Code
CN(C)C1=CC=C(C(C2=CC=C(N(C)C)C=C2)C3=CC([N+]([O-])=O)=CC=C3Cl)C=C1
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
More Info
Biological target:
AL082D06 is a nonsteroidal glucocorticoid receptor (GR) antagonist.
In vitro activity:
D06 was tested for antagonist effects in cell-based models of transcriptional activation. D06 antagonized steroid-mediated induction of glutamine synthetase RNA in MG63 cells and TAT enzyme in human skin fibroblasts (Fig. 4A). D06 was also tested for effects on genes normally repressed by glucocorticoids. Repression was measured using an E-Selectin promoter:luciferase construct. This plasmid contains the E-Selectin gene promoter upstream from the luciferase reporter. TNF and IL-1 strongly induce expression from this plasmid, and glucocorticoids are effective repressors of this induction (Fig. 4B), In contrast, D06 was unable to repress transcription when added alone at any concentration (black squares). However, D06 was able to fully reverse the repression mediated by Dex at the E-selectin promoter. D06 was also capable of partially inhibiting Dex-mediated repression of IL-6 and collagenase protein production from untransfected human skin fibroblast cells using endogenous receptors. In summary, D06 can act to inhibit both transcriptional activation and repression by receptor in a variety of cell types on a variety of genes. Reference: Mol Endocrinol. 2003 Jan;17(1):117-27. https://academic.oup.com/mend/article/17/1/117/2741828
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 6.3 15.25
DMF 10.0 24.40
DMF:PBS (pH 7.2) (1:2) 0.3 0.81
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 409.91 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. 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. doi: 10.1210/me.2002-0010. PMID: 12511611.
In vitro protocol:
1. 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. doi: 10.1210/me.2002-0010. PMID: 12511611.
In vivo protocol:
TBD
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.