Home Endocrinology & Hormones Glucocorticoid Receptor agonist Loteprednol etabonate For research use only.

Loteprednol etabonate

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

Loteprednol etabonate Chemical Structure

Loteprednol etabonate Chemical Structure

CAS No. 82034-46-6

Purity & Quality Control

Loteprednol etabonate Related Products

Biological Activity

Description Loteprednol etabonate is a potent glucocorticoid receptor agonist, used in treatment of inflammation of the eye due to allergies.
Targets
Glucocorticoid receptor [1]
In vitro
In vitro Loteprednol possesses a metabolically labile function, the 17beta-ester, that is designed to be rapidly deactivated in the systemic circulation. Loteprednol etabonate 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. [1]
In Vivo
In vivo Loteprednol etabonate administrated directly into the joint effectively blocks the inflammatory response. Loteprednol etabonate prevents the adverse inflammatory effects of antigen action in a rabbit acute experimental model for arthritis. [2] Loteprednol etabonate (LE) (oral) reaches the upper GI tract effectively, but not the colon, due to absorption and/or decomposition in rats. [3] Loteprednol etabonate (LE) shows a rapid, dose-dependent elimination with a total blood clearance (CLtotal) of higher than 60 ml/min/kg in rats. Loteprednol etabonate absorbes systemically, after topical administration, can be rapidly transformed to the inactive metabolites, and eliminates from the body mainly through the bile and urine. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03063489 Completed
Eye Pain
Bausch Health Americas Inc.
 February 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 466.95 Formula

C24H31ClO7
CAS No. 82034-46-6 SDF Download Loteprednol etabonate SDF
Smiles CCOC(=O)OC1(CCC2C1(CC(C3C2CCC4=CC(=O)C=CC34C)O)C)C(=O)OCCl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 93 mg/mL ( (199.16 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh 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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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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