GB-110 is a potent, orally active, and nonpeptidicprotease activated receptor2 (PAR2)agonist. GB-110 selectively induces PAR2-mediated intracellular Ca²⁺release in HT29 cells with anEC₅₀of 0.28 μM^[1].

Protease activated receptor 2^[1]

In an intracellular Ca²⁺(iCa²⁺) mobilization assay using HT29 colon cancer cells, GB110 (EC₅₀240±20 nM; pEC₅₀6.7±0.05) is equipotent with the peptide agonist 2f-LIGRLO-NH2 (EC₅₀210±30 nM; pEC₅₀6.6±0.05), 10-fold more potent than SLIGRL-NH2, but ~35-fold less potent than trypsin (EC₅₀6±0.5 nM; pEC₅₀8.2±0.8)^[2].

608.77

C₃₃H₄₈N₆O₅

1252806-70-4

Room temperature in continental US; may vary elsewhere.

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