1252806-86-2

1252806-86-2 structure

Name: GB-83
Chemical Name: N-[(2S)-3-Cyclohexyl-1-{[(2S,3S)-1-(2,3-dihydro-1'H-spiro[indene- 1,4'-piperidin]-1'-yl)-3-methyl-1-oxo-2-pentanyl]amino}-1-oxo-2-p ropanyl]-1,2-oxazole-5-carboxamide
CAS Number: 1252806-86-2
Molecular Formula: C₃₂H₄₄N₄O₄
Molecular Weight: 548.71600
Catalog: Signaling Pathways GPCR/G Protein Protease-Activated Receptor (PAR)
Create Date: 2017-06-14 05:52:13
Modify Date: 2024-01-13 13:40:41
GB83 is a potent PAR2 antagonist. GB83 reverses neutrophil elastase‐induced synovitis and pain. GB83 blocks the effect of MET-1 supernatant on NG neurons[1].

Name	N-[(2S)-3-Cyclohexyl-1-{[(2S,3S)-1-(2,3-dihydro-1'H-spiro[indene- 1,4'-piperidin]-1'-yl)-3-methyl-1-oxo-2-pentanyl]amino}-1-oxo-2-p ropanyl]-1,2-oxazole-5-carboxamide
Synonyms	5-isoxazoyl-Cha-Ile-spiroindane-1,4'-piperidine Pentanoic acid,5-isothiocyanato 5-Isothiocyanatovaleriansaeure 5-Isothiocyanato-pentanoic acid GB-83

Description	GB83 is a potent PAR2 antagonist. GB83 reverses neutrophil elastase‐induced synovitis and pain. GB83 blocks the effect of MET-1 supernatant on NG neurons[1].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Protease-Activated Receptor (PAR) Research Areas >> Inflammation/Immunology Research Areas >> Neurological Disease
Target	PAR2
In Vitro	GB83 (10 µM) blocks the effect of MET-1 (microbial ecosystem therapeutic-1) supernatant on nodose ganglion (NG) neurons[2].
In Vivo	GB83 (5 µg; i.p.) reverses neutrophil elastase‐induced synovitis and pain in PAR2 KO mice[1]. Animal Model: 8-14 weeks, 20-30 g male C57Bl/6 mice (PAR2 KO mice)[1] Dosage: 5 µg Administration: I.p.; 3 times at 10 min before and 110 and 230 min after neutrophil elastase administered Result: Significantly blocked the neutrophil elastase induced increase in vascular perfusion, as well as the number of rolling adherent leukocytes, and also significantly attenuated hindpaw allodynia.
References	[1]. Muley MM, et al. Neutrophil elastase induces inflammation and pain in mouse knee joints via activation of proteinase-activated receptor-2. Br J Pharmacol. 2016 Feb;173(4):766-77. [2]. Pradhananga S, et al. Protease-dependent excitation of nodose ganglion neurons by commensal gut bacteria. J Physiol. 2020 Jun;598(11):2137-2151.