BMS-791826

Cat. No.: HY-165370: Data Sheet Handling Instructions
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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.

BMS-791826 Chemical Structure

CAS No. : 1008116-73-1

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Biological Activity
Purity & Documentation
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Description

Cellular Effect

Cell Line	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]

Clinical Trial

Molecular Weight

531.60

Formula

C₂₈H₂₆FN₅O₃S

CAS No.

1008116-73-1

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Hu Y, et al. Development of a Molecular Signature to Monitor Pharmacodynamic Responses Mediated by In Vivo Administration of Glucocorticoids. Arthritis Rheumatol. 2018 Aug;70(8):1331-1342. [Content Brief]

BMS-791826 Related Classifications

Inflammation/Immunology

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The dilution calculator equation

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-7918261008116-73-1BMS791826BMS 791826Glucocorticoid ReceptorAP-1NF-κBActivator Protein 1Nuclear factor-κBNuclear factor-kappaBrheumatoid arthritisinflammatory bowel diseasepsoriasisasthmaSK-N-MCA549 cellsInhibitorinhibitorinhibit

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