GB-88

1416435-96-5

546.70

H2O : < 0.1 mg/mL (insoluble); DMSO : 31.25 mg/mL (57.16 mM; Need ultrasonic)

GPCR/G Protein

GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca²⁺ release with an IC₅₀ of 2 uM^[1]. IC50 & Target: PAR2^[1] In Vitro: GB-88 inhibits iCa²⁺ release induced in HT29 cells by trypsin, 2f-LIGRLO-NH2 and GB110 (PAR2 agonists). And antagonism by GB-88 is agonist dependent^[1].
In Vivo: GB-88 (10 mg/kg, p.o. in olive oil) is both orally active and anti-inflammatory in vivo, with specific antagonist activity against four structurally and mechanistically different PAR2 agonists (2f-LIGRLO-NH2, trypsin, SLIGRL-NH2 and GB110)^[1].
GB-88 inhibits PAR2-induced acute inflammation in vivo^[1].