Loteprednol etabonate
Catalog No.S1669
Molecular Weight(MW): 466.95
Loteprednol etabonate is a potent glucocorticoid receptor agonist, used in treatment of inflammation of the eye due to allergies.
Purity & Quality Control
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. | |
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| 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] |
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| 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) |
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| 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 |
Bio Calculators
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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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