1. Immunology/Inflammation Vitamin D Related/Nuclear Receptor NF-κB
  2. Glucocorticoid Receptor AP-1 NF-κB
  3. BMS-791826

BMS-791826 是选择性糖皮质激素受体 (glucocorticoid receptor) 调节剂。BMS-791826 有效结合糖皮质激素受体,并有效抑制 AP-1NF-κB 依赖的报告基因。BMS-791826 可用于炎症性疾病研究。

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BMS-791826

BMS-791826 Chemical Structure

CAS No. : 1008116-73-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
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]
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]
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]
分子量

531.60

Formula

C28H26FN5O3S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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.

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产品名称:
BMS-791826
目录号:
HY-165370
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