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Table 1 Inhibitors and their main effects

From: Preparation and in vivo and ex vivo studies of sirolimus nano-in-situ gel ophthalmic formulation

Inhibitor

Concentration

Primary Action

Chlorpromazine

6 µg/mL

Inhibitor of clathrin-mediated endocytosis

Indomethacin

100 µM

Inhibitor of cell membrane caveolae-like invaginations-mediated endocytosis

Heparin

100 µg/mL

Specific inhibitor of heparan sulfate proteoglycans

Amiloride

10 µM

Specific inhibitor of macrophagocytosis

Sodium azide

0.10%

General inhibitor of endocytosis process

Hypertonic sucrose

0.45 M

Inhibitor of lattice protein-mediated endocytosis through K+depleting effects

Methyl-β-cyclodextrin

10 mM

Cholesterol depleting agent capable of inhibiting lipid raft/envelope cellar-dependent cytosis

Chloroquine

125 mM

Destroys endosomes and lysosomes, prevents endosomal acidification, and causes swelling of endosomes and lysosomes

Mycophenolate

10 µg/mL

Inhibits lipid raft/periplasmic caveolae-like invagination-dependent endocytosis via cholesterol chelation