Size | Price | Stock | Qty |
---|---|---|---|
2mg |
|
||
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
Other Sizes |
|
Purity: ≥98%
AL082D06 (formerly known as D-06), is a nonsteroidal glucocorticoid receptor (GR) antagonist which is characterized by a tri-aryl methane core chemical structure. 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. Once bound, however, AL082D06 fails to induce critical conformational changes in the receptor necessary for agonist activity.
ln Vitro |
GR is selectively bound by AL 082D06 (D06) with nanomolar affinity. When half-maximal DEX concentration was used to stimulate the MMTV:Luc reporter, transcriptional activation decreased in a dose-dependent manner upon the addition of AL 082D06. Several glucocorticoid-responsive promoter-reporter systems are used by AL 082D06, including a less complex one made up of isolated glucocorticoid-responsive element (GRE) sequences and the 3-kb tyrosine aminotransferase (TAT) promoter. promoter to sabotage the work of reporters. With nanomolar affinity, AL 082D06 faces off against 3H-Dex for baculovirus-expressed GR. Using the appropriate receptor and tritiated ligand (>2500 nM), similar structural binding assays revealed no affinity for AL 082D06 for other intracellular receptors (AR, ER, PR, and MR). Progesterone, androgens, mineralocorticoids, retinoic acid, glucocorticoids, and estrogen receptors are not activated by AL 082D06. When tested against other steroid receptors, AL 082D06 is much less effective than the reference antagonist used as a control, despite having a very strong ability to oppose GR activity [1].
|
||
---|---|---|---|
ln Vivo |
|
||
Animal Protocol |
|
||
References |
[1]. Miner JN, et al. A nonsteroidal glucocorticoid receptor antagonist. Mol Endocrinol. 2003 Jan;17(1):117-27
|
Molecular Formula |
C23H24CLN3O2
|
|
---|---|---|
Molecular Weight |
409.91
|
|
CAS # |
256925-03-8
|
|
Related CAS # |
|
|
SMILES |
CN(C)C1=CC=C(C(C2=CC=C(N(C)C)C=C2)C3=CC([N+]([O-])=O)=CC=C3Cl)C=C1
|
|
Chemical Name |
4,4'-((2-chloro-5-nitrophenyl)methylene)bis(N,N-dimethylaniline)
|
|
Synonyms |
AL-082D06; AL082D06; AL 082D06; D-06; D06; D 06
|
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.