1. GPCR/G Protein
  2. Glucocorticoid Receptor
  3. AL 082D06

AL 082D06 (Synonyms: D06; D-06)

Cat. No.: HY-15709 Purity: 98.92%
Handling Instructions

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

For research use only. We do not sell to patients.

AL 082D06 Chemical Structure

AL 082D06 Chemical Structure

CAS No. : 256925-03-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 462 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

Ki: 210 nM (GR)[1]

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].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 7.5 mg/mL (18.30 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 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 0.2440 mL 1.2198 mL 2.4396 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

409.91

Formula

C₂₃H₂₄ClN₃O₂

CAS No.

256925-03-8

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-]

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.92%

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Product Name:
AL 082D06
Cat. No.:
HY-15709
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AL 082D06

Cat. No.: HY-15709