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Loteprednol etabonate Glucocorticoid Receptor agonist

Cat.No.S1669

Loteprednol etabonate is a potent glucocorticoid receptor agonist, used in treatment of inflammation of the eye due to allergies.
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Quality Control

Batch: Purity: 100.00%
100.00

Solubility

In vitro
Batch:

DMSO : 93 mg/mL (199.16 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

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In vivo
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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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Chemical Information, Storage & Stability

Molecular Weight 466.95 Formula

C24H31ClO7

Storage (From the date of receipt)
CAS No. 82034-46-6 Download SDF Storage of Stock Solutions

Synonyms N/A SMILES CCOC(=O)OC1(CCC2C1(CC(C3C2CCC4=CC(=O)C=CC34C)O)C)C(=O)OCCl

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Mechanism of Action

Targets/IC50/Ki
Glucocorticoid receptor
In vitro
Loteprednol etabonate possesses a metabolically labile function, the 17beta-ester, that is designed to be rapidly deactivated in the systemic circulation. This compound exhibits a binding affinity which is 4.3 times that of dexamethasone, both compounds having a Hill factor close to 1 whereas PJ90 and PJ91 does not show any affinity to the receptor.
In vivo
Loteprednol etabonate administrated directly into the joint effectively blocks the inflammatory response. This compound prevents the adverse inflammatory effects of antigen action in a rabbit acute experimental model for arthritis. It (oral) reaches the upper GI tract effectively, but not the colon, due to absorption and/or decomposition in rats. This chemical shows a rapid, dose-dependent elimination with a total blood clearance (CLtotal) of higher than 60 ml/min/kg in rats. It absorbes systemically, after topical administration, can be rapidly transformed to the inactive metabolites, and eliminates from the body mainly through the bile and urine.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/7667193/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-03-27)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07496060 COMPLETED
Anterior Chamber Granulomatous Uveitis
Fayoum University
2025-08-10 PHASE4
NCT05542381 COMPLETED
Age-Related Macular Degeneration
Virginia Polytechnic Institute and State University
2022-12-22
NCT05136443 COMPLETED
Corneal Endothelial Dystrophy; Corneal Edema
Price Vision Group
2021-11-23 PHASE4
NCT07090044 COMPLETED
Vein Occlusion; Macular Degeneration Choroidal Neovascularization; Macular Edema; Diabetic Retinopathy
Retina Research Institute, LLC
2021-08-20 PHASE4
NCT05322148 COMPLETED
Dry Eye
Research Insight LLC
2022-06-03 PHASE3
NCT04555694 COMPLETED
Dry Eye
Thomas Chester, OD
2020-10-01 PHASE4

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