tcsc8047 Larazotide acetate

Larazotide acetate is a synthetic peptide that functions as a tight junction regulator and reverses leaky junctions to their normally closed state.

IC50 & Target: Paracellular permeability^[1]

In Vitro: Larazotide acetate inhibits the redistribution and rearrangement of zonula occludens-1 (ZO-1) and actin caused by AT-1002 and gliadin fragments in Caco-2 and IEC6 cells. Larazotide acetate inhibits the AT-1002-induced TEER reduction and TJ opening in Caco-2 cells. Larazotide acetate inhibits the translocation of a gliadin 13-mer peptide, which has been implicated in celiac disease, across Caco-2 cell monolayers. Further, apically applied Larazotide acetate inhibits the increase in TJ permeability elicited by basolaterally applied cytokines^[1].

In Vivo: When tested in vivo in gliadin-sensitized HLA-HCD4/DQ8 double transgenic mice, larazotide acetate inhibits gliadin-induced macrophage accumulation in the intestine and preserved normal tight junction structure^[1].