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Budesonide Glucocorticoid Receptor agonist

Name: Budesonide
SKU: S1286
Availability: InStock
Rating: 5 (9 reviews)

Cat.No.S1286

Budesonide(Labazenit) is a glucocorticoid steroid for the treatment of asthma, non-infectious rhinitis.

Chemical Structure

Molecular Weight: 430.53

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Estrogen/progestogen Receptor Adrenergic Receptor GPR Androgen Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR PGES Aromatase CCK receptor 5-alpha Reductase Mineralocorticoid Receptor GHSR SSTR TSH Receptor GNRH Receptor PGDS
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Chemical Information, Storage & Stability

Molecular Weight	430.53	Formula	C₂₅H₃₄O₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	51333-22-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.300mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 86 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Glucocorticoid receptor ^[1]
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. ^[1] 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. ^[2] 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. ^[3]
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. ^[4] 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. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/10553092/ [2] https://pubmed.ncbi.nlm.nih.gov/11502275/ [3] https://pubmed.ncbi.nlm.nih.gov/10442524/ [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 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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