research use only
Cat.No.S1286
| Related Targets | Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR |
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| Other Glucocorticoid Receptor Inhibitors | Corticosterone AL082D06 (20S)-Protopanaxatriol Cortodoxone |
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In vitro |
DMSO
: 86 mg/mL
(199.75 mM)
Ethanol : 10 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 430.53 | Formula | C25H34O6 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 51333-22-3 | Download SDF | Storage of Stock Solutions |
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| Synonyms | Labazenit | Smiles | CCCC1OC2CC3C4CCC5=CC(=O)C=CC5(C4C(CC3(C2(O1)C(=O)CO)C)O)C | ||
| Targets/IC50/Ki |
Glucocorticoid receptor
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| In vitro |
Budesonide effectively inhibits production of eotaxin and RANTES protein although this compound inhibits the expression of chemokine mRNA to a variable extent in the human bronchial epithelial cell line BEAS-2B and in primary human bronchial epithelial cells. It inhibits both RANTES- and eotaxin promoter-driven reporter gene activity in the human bronchial epithelial cell line BEAS-2B and in primary human bronchial epithelial cells. This chemical also selectively accelerates the decay of eotaxin and MCP-4 mRNA in the human bronchial epithelial cell line BEAS-2B and in primary human bronchial epithelial cells. It time- and protein synthesis-dependently reduces VEGF secretion and VEGF mRNA expression in both cell types and these effects are inhibited by mifepristone (RU 486), a glucocorticoid receptor antagonist, suggesting that this compound reduces VEGF secretion and expression through its glucocorticoid receptor-mediated action. It causes a dose-dependent, almost total, inhibition of swine dust-induced IL-6 and IL-8 release from epithelial cells and LPS-induced IL-6 and TNF-alpha from alveolar macrophages. |
| In vivo |
Budesonide totally prevents the increased production of TNF-alpha, interleukin (IL)-1beta, IL-6, and monocyte chemoattractive protein (MCP)-1 after LPS challenge at both low (2.5 mg/mL/kg) and high (50 mg/mL/kg) concentrations in rats. This compound exerts its effects of chemoprevention through growth arrest via Mad2/3 and through apoptosis via Bim/Blk and, by inference, caspase-8/9 in A/J mice. |
References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05341401 | Not yet recruiting | Ulcerative Colitis Chronic |
Assiut University |
June 2022 | Phase 2|Phase 3 |
| NCT05148312 | Completed | Pharmacokinetics |
Aquilon Pharmaceuticals S.A. |
November 12 2021 | Phase 1 |
| NCT04342039 | Active not recruiting | Epigenetic Effects of Intranasal Steroids|Environmental Exposure |
University of British Columbia|Genome British Columbia|Johnson & Johnson Consumer Inc. (J&JCI) |
January 7 2021 | Phase 4 |
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