GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca release with an IC50 of 2 µM.
IC50&Target
PAR2
体外研究
GB-88 inhibits iCa release induced in HT29 cells by trypsin, 2f-LIGRLO-NH2 and GB110 (PAR2 agonists). And antagonism by GB-88 is agonist dependent.
体内研究
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).
GB-88 inhibits PAR2-induced acute inflammation in vivo.
Animal Model:
Male Wistar rats (8–9 weeks)
Dosage:
10 mg/kg
Administration:
Oral gavage in olive oil
Result:
Was 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).
分子式
C32H42N4O4
分子量
546.70
CAS号
1416435-96-5
运输条件
Room temperature in continental US; may vary elsewhere.