BMS-791826
BMS-791826 is a selective glucocorticoid receptor modulator. BMS-791826 effectively binds to glucocorticoid receptors and effectively inhibits AP-1 and NF-κB-dependent reporter. BMS-791826 can be used in the research of inflammatory diseases.
For research use only. We do not sell to patients.
- CAS No.: 1008116-73-1
- Formula: C28H26FN5O3S
- Molecular Weight:531.60
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All AP-1 Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | EC50 |
>5 μM
Compound: 37, BMS-791826
|
Agonist activity at human mineralocorticoid receptor expressed in human A549 cells by fluorescence polarization assay
Agonist activity at human mineralocorticoid receptor expressed in human A549 cells by fluorescence polarization assay
|
[PMID: 21899328] |
| A549 | EC50 |
17.7 nM
Compound: 37, BMS-791826
|
Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 response element by luciferase reporter gene assay
Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 response element by luciferase reporter gene assay
|
[PMID: 21899328] |
| A549 | EC50 |
6.89 nM
Compound: 37, BMS-791826
|
Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
|
[PMID: 21899328] |
| HeLa | EC50 |
113.4 nM
Compound: 37, BMS-791826
|
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as inhibition of GAL4-DBD after 20 hrs by luciferase reporter gene assay
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as inhibition of GAL4-DBD after 20 hrs by luciferase reporter gene assay
|
[PMID: 21899328] |
| HeLa | EC50 |
98.5 nM
Compound: 37, BMS-791826
|
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs by luciferase reporter gene assay
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs by luciferase reporter gene assay
|
[PMID: 21899328] |
| Huh-7 | EC50 |
88 nM
Compound: 37, BMS-791826
|
Transactivation activity at glucocorticoid receptor alpha human 13D3/Huh7 cells assessed as induction of TAT activity after 4 hrs by spectrophotometry
Transactivation activity at glucocorticoid receptor alpha human 13D3/Huh7 cells assessed as induction of TAT activity after 4 hrs by spectrophotometry
|
[PMID: 21899328] |
| MG-63 | EC50 |
207 nM
Compound: 37, BMS-791826
|
Induction of glutamine synthase expression in human MG63 cells after overnight incubation by spectrophotometry
Induction of glutamine synthase expression in human MG63 cells after overnight incubation by spectrophotometry
|
[PMID: 21899328] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1008116-73-1
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Molecular Weight 531.60
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Formula C28H26FN5O3S
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SMILES
O=C(NC1=NN=CS1)C(C)([C@@H]2C3=CC=C(C4=CC(F)=C(C=C4)C(N(C)CC)=O)N=C3OC5=CC=CC=C52)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)