Dexamethasone fluorescein 

Dexamethasone fluorescein is a fluorescently labeled steroid conjugate that binds to glucocorticoid receptors. Dexamethasone fluorescein binds to glucocorticoid receptors. Dexamethasone fluorescein serves as a marker for evaluating the delivery of drugs via subconjunctival injection and intratympanic administration. Sustained transscleral diffusion is achieved when Dexamethasone fluorescein is delivered via fibrin sealant. Dexamethasone fluorescein can be used to investigate the binding and localization of glucocorticoid receptors^[1][2][3].

Dexamethasone fluorescein (10^-4 M; 6 h) exhibits a steady-state permeability constant (K_trans) of 1.64 × 10^-6 cm/sec in human scleral sections, which is significantly lower than the permeability of more hydrophilic compounds fluorescein and methotrexate-fluorescein^[1].
Dexamethasone fluorescein (100 μM; 10 hr) exhibits steady, gradual release from a fibrin sealant depot over 10 hours, with 4.0% of the initial amount released by the end of the period^[3].
Dexamethasone fluorescein (100 μM; 24 hr) delivered via fibrin sealant shows sustained transscleral diffusion across excised human scleral sections over 24 hours, with 1% of the initial amount diffused, an apparent scleral permeability of 1.58×10^-7 cm/s, and minimal tissue uptake of 3%^[3].
Dexamethasone fluorescein (1.0×10^-4 M; 24 hr) delivered in balanced salt solution (BSS) shows rapid transscleral diffusion across excised human scleral sections over 24 hours, with 18% of the initial amount diffused, an apparent scleral permeability of 2.57×10^-6 cm²/s, and substantial tissue uptake of 23%^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Dexamethasone fluorescein (1 mM; intratympanic; single application; 60-minute application period) shows minimal entry into guinea pig perilymph alone, but entry is significantly increased by co-administration with permeation enhancers, with 4% benzyl alcohol producing the greatest effect^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

840.98

C₄₅H₄₅FN₂O₉S₂

216854-76-1

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Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Cruysberg LP, et al. In vitro human scleral permeability of fluorescein, dexamethasone-fluorescein, methotrexate-fluorescein and rhodamine 6G and the use of a coated coil as a new drug delivery system. J Ocul Pharmacol Ther. 2002 Dec;18(6):559-69.  [Content Brief]

  [2]. Li W, et al. Permeation Enhancers for Intratympanically-applied Drugs Studied Using Fluorescent Dexamethasone as a Marker. Otology & neurotology : official publication of the American Otological Society, American Neurotology Society [and] European Academy of Otology and Neurotology. 2018 Jun;39(5):639-647.  [Content Brief]

  [3]. Cruysberg LP, et al. In vitro sustained human transscleral drug delivery of fluorescein-labeled dexamethasone and methotrexate with fibrin sealant. Current eye research. 2005 Aug;30(8):653-60.  [Content Brief]