GB-110 (hydrochloride)

645.23

DMSO : 125 mg/mL (193.73 mM; Need ultrasonic)

GPCR/G Protein

GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca²⁺ release in HT29 cells with an EC₅₀ of 0.28 uM^[1]. IC50 & Target: Protease activated receptor 2^[1] In Vitro: In an intracellular Ca²⁺ (iCa²⁺) mobilization assay using HT29 colon cancer cells, GB110 (EC₅₀ 240+/-20 nM; pEC₅₀ 6.7+/-0.05) is equipotent with the peptide agonist 2f-LIGRLO-NH2 (EC₅₀ 210+/-30 nM; pEC₅₀ 6.6+/-0.05), 10-fold more potent than SLIGRL-NH2, but ca.35-fold less potent than trypsin (EC₅₀ 6+/-0.5 nM; pEC₅₀ 8.2+/-0.8)^[2].