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1252806-86-2

1252806-86-2 structure
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: 2025-08-27 21:44:26
  • 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
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.

Molecular Formula C32H44N4O4
Molecular Weight 548.71600
Exact Mass 548.33600
PSA 108.03000
LogP 5.95000
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