product name Loteprednol etabonate
Description: Loteprednol etabonate, the esther of Loteprednol, is a potent glucocorticoid receptor agonist, it is used in treatment of inflammation of the eye due to allergies. 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.
References: J Steroid Biochem Mol Biol. 1991 Feb;38(2):149-54; Pharmazie. 1999 Jan;54(1):58-61.
466.95
Formula
C24H31ClO7
CAS No.
82034-46-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 93 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (8.6 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19422481
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. Loteprednol etabonate (LE) (oral) reaches the upper GI tract effectively, but not the colon, due to absorption and/or decomposition in rats. 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Steroid Biochem Mol Biol. 1991 Feb;38(2):149-54; Pharmazie. 1999 Jan;54(1):58-61. |
