| Bioactivity | GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 µM[1]. | ||||||||||||
| Target | PAR2 | ||||||||||||
| Invitro | 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]. Animal Model: | ||||||||||||
| Name | GB-88 | ||||||||||||
| CAS | 1416435-96-5 | ||||||||||||
| Formula | C32H42N4O4 | ||||||||||||
| Molar Mass | 546.70 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |