For research use only. Not for therapeutic Use.
GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM[1].
In an intracellular Ca2+ (iCa2+) mobilization assay using HT29 colon cancer cells, GB110 (EC50 240±20 nM; pEC50 6.7±0.05) is equipotent with the peptide agonist 2f-LIGRLO-NH2 (EC50 210±30 nM; pEC50 6.6±0.05), 10-fold more potent than SLIGRL-NH2, but ~35-fold less potent than trypsin (EC50 6±0.5 nM; pEC50 8.2±0.8)[2].
| Catalog Number | I046082 |
| Synonyms | N-[(2S)-1-[[(2S,3S)-1-[[3-[4-(aminomethyl)piperidine-1-carbonyl]phenyl]methylamino]-3-methyl-1-oxopentan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]-1,2-oxazole-5-carboxamide;hydrochloride |
| Molecular Formula | C33H49ClN6O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C33H48N6O5.ClH/c1-3-22(2)29(38-30(40)27(19-23-8-5-4-6-9-23)37-31(41)28-12-15-36-44-28)32(42)35-21-25-10-7-11-26(18-25)33(43)39-16-13-24(20-34)14-17-39;/h7,10-12,15,18,22-24,27,29H,3-6,8-9,13-14,16-17,19-21,34H2,1-2H3,(H,35,42)(H,37,41)(H,38,40);1H/t22-,27-,29-;/m0./s1 |
| InChIKey | QHVXUZNJSKXTQC-PKPQYKQISA-N |
| SMILES | CCC(C)C(C(=O)NCC1=CC(=CC=C1)C(=O)N2CCC(CC2)CN)NC(=O)C(CC3CCCCC3)NC(=O)C4=CC=NO4.Cl |
| Reference | [1]. Barry GD, et al. Novel agonists and antagonists for human protease activated receptor 2. J Med Chem. 2010 Oct 28;53(20):7428-40. [2]. 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. |
