For research use only. Not for therapeutic Use.
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].
| Catalog Number | I019183 |
| CAS Number | 1416435-96-5 |
| Synonyms | N-[(2S)-3-cyclohexyl-1-[[(2S,3S)-3-methyl-1-oxo-1-spiro[indene-1,4′-piperidine]-1′-ylpentan-2-yl]amino]-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamide |
| Molecular Formula | C32H42N4O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C32H42N4O4/c1-3-22(2)28(31(39)36-19-16-32(17-20-36)15-13-24-11-7-8-12-25(24)32)35-29(37)26(21-23-9-5-4-6-10-23)34-30(38)27-14-18-33-40-27/h7-8,11-15,18,22-23,26,28H,3-6,9-10,16-17,19-21H2,1-2H3,(H,34,38)(H,35,37)/t22-,26-,28-/m0/s1 |
| InChIKey | DCUDDCGUKZLQLN-MCOVPRHSSA-N |
| SMILES | CCC(C)C(C(=O)N1CCC2(CC1)C=CC3=CC=CC=C23)NC(=O)C(CC4CCCCC4)NC(=O)C5=CC=NO5 |
| 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. |
