Loteprednol etabonate

Catalog No.S1669

Loteprednol etabonate Chemical Structure

Molecular Weight(MW): 466.95

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

Size Price Stock Quantity  
In DMSO USD 140 In stock
USD 60 In stock
USD 360 In stock
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Choose Selective Glucocorticoid Receptor Inhibitors

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

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 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]

Protocol

Solubility (25°C)

In vitro DMSO 93 mg/mL (199.16 mM)
Ethanol 4 mg/mL (8.56 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 466.95
Formula

C24H31ClO7

CAS No. 82034-46-6
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02208297 Completed Inflammation|Pain|Cataract Bausch & Lomb Incorporated September 2014 Phase 3
NCT02218827 Unknown status Dry Eye Meir Medical Center September 2014 --
NCT02106377 Unknown status Dry Eye Syndrome Massachusetts Eye and Ear Infirmary February 2014 --
NCT02028312 Withdrawn Dry Eye Disease Edward Holland, MD|Holprovision January 2014 Phase 4
NCT01996839 Completed Inflammation|Pain|Cataract Bausch & Lomb Incorporated December 2013 Phase 3
NCT01475643 Recruiting Cataract Bausch & Lomb Incorporated July 2013 Phase 3

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID