AL082D06
AL 082D06
CAS: 256925-03-8
Molecular Formula: C23H24ClN3O2
AL082D06 - Names and Identifiers
AL082D06 - Physico-chemical Properties
| Molecular Formula | C23H24ClN3O2 |
| Molar Mass | 409.91 |
| Density | 1.232±0.06 g/cm3(Predicted) |
| Boling Point | 543.7±50.0 °C(Predicted) |
| Solubility | DMSO: 7.5 mg/mL |
| pKa | 5.36±0.24(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | 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 3 H-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. |
AL082D06 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.44 ml | 12.198 ml | 24.396 ml |
| 5 mM | 0.488 ml | 2.44 ml | 4.879 ml |
| 10 mM | 0.244 ml | 1.22 ml | 2.44 ml |
| 5 mM | 0.049 ml | 0.244 ml | 0.488 ml |
Last Update：2024-01-02 23:10:35
AL082D06 - Reference Information
| biological activity | AL082D06 is a non-steroid glucocorticoid receptor antagonist, but has no significant binding affinity for its highly related receptors such as mineralocorticoid, androgen, estrogen and progesterone. |
| target | TargetValue Glucocorticoid receptor () 210 nM(Ki) |
| Target | Value |
| Glucocorticoid receptor () | 210 nM(Ki) |
| in vitro study | AL 082D06 (D06) binds specifically to GR with nanomolar affinity. Addition of AL 082D06 cause 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 3 H-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 say 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. |
Last Update：2024-04-10 22:29:15
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