GB-88 是一种口服、选择性的非肽类 PAR2 拮抗剂，可抑制 PAR2 介导的 Ca2+ 的释放，IC50 值为 2 µM。
货号:ajcx39584
CAS:1416435-96-5
分子式:C32H42N4O4
分子量：546.7
溶解度:DMSO : 31.25 mg/mL (57.16 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 µM[1].

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].

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].

[1]. Suen JY, et al. Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110). Br J Pharmacol. 2012 Mar;165(5):1413-23.