| Identification | Back Directory | [Name]
GB 83 | [CAS]
1252806-86-2 | [Synonyms]
GB 83
GB-83
(GB83)
5-Isoxazolecarboxamide, N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S,2S)-1-[(2,3-dihydrospiro[1H-indene-1,4'-piperidin]-1'-yl)carbonyl]-2-methylbutyl]amino]-2-oxoethyl]- | [Molecular Formula]
C32H44N4O4 | [MDL Number]
MFCD20926417 | [MOL File]
1252806-86-2.mol | [Molecular Weight]
548.72 |
| Chemical Properties | Back Directory | [Boiling point ]
807.6±65.0 °C(Predicted) | [density ]
1.20±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
12.12±0.46(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
GB83 is a serum stablepotent and selective antagonist of human protease activated receptor 2 (PAR2)(IC50 = 2 μM) th at reversibly inhibit PAR2 activation by both proteases and PAR2 agonists. GB83 prevented upregulation of PARsICAM-1LOX-1IL-8and activation of MAP kinases by coagulation factor X (FXa) in atrial tissue slices | [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. |
| [IC 50]
PAR2 | [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. DOI:10.1111/bph.13237
[2] Pradhananga S, et al. Protease-dependent excitation of nodose ganglion neurons by commensal gut bacteria. J Physiol. 2020 Jun;598(11):2137-2151. DOI:10.1113/JP279075 |
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Merck KGaA
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