| Identification | Back Directory | [Name]
GB-88 | [CAS]
1416435-96-5 | [Synonyms]
GB-88 Spiro[1H-indene-1,4'-piperidine], 1'-[3-cyclohexyl-N-(5-isoxazolylcarbonyl)-L-alanyl-L-isoleucyl]- | [Molecular Formula]
C32H42N4O4 | [MDL Number]
MFCD29920338 | [MOL File]
1416435-96-5.mol | [Molecular Weight]
546.7 |
| Hazard Information | Back Directory | [Uses]
GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 μM[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: | Male Wistar rats (8–9 weeks)[1] | | 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). |
| [IC 50]
PAR2: 2 μM (IC50) | [References]
[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. DOI:10.1111/j.1476-5381.2011.01610.x |
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