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Budesonide Glucocorticoid Receptor Agonist

Cat.No.: S1286

Budesonide (Labazenit) is a glucocorticoid steroid for the treatment of asthma, non-infectious rhinitis.
Budesonide Glucocorticoid Receptor Agonist Chemical Structure

Chemical Structure

Molecular Weight: 430.53

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Quality Control

Batch: Purity: 99.97%
99.97

Chemical Information, Storage & Stability

Molecular Weight 430.53 Formula

C25H34O6

Storage (From the date of receipt)
CAS No. 51333-22-3 Download SDF Storage of Stock Solutions

Synonyms Labazenit Smiles CCCC1OC2CC3C4CCC5=CC(=O)C=CC5(C4C(CC3(C2(O1)C(=O)CO)C)O)C

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (199.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
Glucocorticoid receptor
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
  • [4] https://pubmed.ncbi.nlm.nih.gov/15967733/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15361829/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-07)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06860542 RECRUITING
Pneumonitis; Immune-related Adverse Event
AHS Cancer Control Alberta
2026-02-10 PHASE2
NCT05976802 NOT_YET_RECRUITING
Ulcerative Colitis
Bausch Health Americas, Inc.
2027-06 PHASE4
NCT07560462 NOT_YET_RECRUITING
Esophageal Stricture
Shaare Zedek Medical Center
2026-05-01
NCT06855043 NOT_YET_RECRUITING
Invasive Mechanical Ventilation; Severe Respiratory Distress Syndrome
University of Wisconsin, Madison
2026-09 PHASE1; PHASE2
NCT06429475 RECRUITING
Asthma
University of KwaZulu
2024-06-06 PHASE3
NCT06076304 RECRUITING
Sinus Infection; Acute Sinusitis
Daniel Merenstein
2023-11-21 PHASE4