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AL 082D06 (D06)

Catalog No.GC32405

AL 082D06 (D06) is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.

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AL 082D06 (D06) Chemical Structure

Cas No.: 256925-03-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$251.00
In stock
2mg
$185.00
In stock
5mg
$278.00
In stock
10mg
$371.00
In stock
50mg
$1,112.00
In stock
100mg
$1,576.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment:

The extract and binding assay buffer consists of 25 mM sodium phosphate, 10 mM potassium fluoride, 10 mM sodium molybdate, 10% glycerol, 1.5 mM EDTA, 2 mM dithiothreitol, 2 mM CHAPS, and 1 mM phenylmethylsulfonyl fluoride (pH 7.4), at room temperature. Intracellular receptors produced in this fashion exhibit reproducible interaction with known ligands at the published affinity. These preparations are subjected to extensive quality control experiments before the assays, covering receptor response, specificity, size, and reference ligand affinity. Receptor assays are performed with a final volume of 250 μL containing from 50-75 μg of extract protein, plus 1-2 nM [3H]Dex at 84 Ci/mmol and varying concentrations of competing ligand (0 to 10 μM). Assays are set up using a 96-well minitube system, and incubations are carried out at 4°C for 18 h. Equilibrium under these conditions of buffer and temperature is achieved by 6-8 h. Nonspecific binding is defined as that binding remaining in the presence of 1000 nM unlabeled Dex. At the end of the incubation period, 200 μL of 6.25% hydroxyapatite are added in wash buffer (binding buffer in the absence of dithiothreitol and phenylmethylsulfonyl fluoride). Specific ligand binding to receptor is determined by a hydroxyapatite-binding assay. Hydroxyapatite absorbs the receptor-ligand complex, allowing for the separation of bound from free radiolabeled ligand. The mixture is vortexed and incubated for 10 min at 4°C and centrifuged, and the supernatant is removed. The hydroxyapatite pellet is washed two times in wash buffer. The amount of receptor-ligand complex is determined by liquid scintillation counting of the hydroxyapatite pellet after the addition of 0.5 mM EcoScint A scintillation cocktail from National Diagnostics[1].

References:

[1]. Miner JN, et al. A nonsteroidal glucocorticoid receptor antagonist. Mol Endocrinol. 2003 Jan;17(1):117-27.

Background

AL 082D06 is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.

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].

[1]. Miner JN, et al. A nonsteroidal glucocorticoid receptor antagonist. Mol Endocrinol. 2003 Jan;17(1):117-27.

Chemical Properties

Cas No. 256925-03-8 SDF
Canonical 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 C23H24ClN3O2 M.Wt 409.91
Solubility DMSO : 7.5 mg/mL (18.30 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.4396 mL 12.1978 mL 24.3956 mL
5 mM 0.4879 mL 2.4396 mL 4.8791 mL
10 mM 0.244 mL 1.2198 mL 2.4396 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 2 reference(s) in Google Scholar.)

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