GB-88 |
| Catalog No.GC65439 |
GB-88 es un antagonista oral selectivo no peptÍdico de PAR2 que inhibe la liberaciÓn de Ca2+ activada por PAR2 con una IC50 de 2 μM.
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Cas No.: 1416435-96-5
Sample solution is provided at 25 µL, 10mM.
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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.
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