WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 527107

CAS#: 1252806-86-2

Description: GB83 is a selective antagonist of human protease activated receptor 2 (PAR2).

Chemical Structure

CAS# 1252806-86-2

Theoretical Analysis

MedKoo Cat#: 527107
Name: GB83
CAS#: 1252806-86-2
Chemical Formula: C32H44N4O4
Exact Mass: 548.34
Molecular Weight: 548.728
Elemental Analysis: C, 70.04; H, 8.08; N, 10.21; O, 11.66

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: GB83; GB 83; GB-83

IUPAC/Chemical Name: N-((S)-3-Cyclohexyl-1-((2S,3S)-1-(2,3-dihydrospiro[indene-1,4'-piperidine]-1'-yl)-3-methyl-1-oxopentan-2-ylamino)-1-oxopropan-2-yl)isoxazole-5-carboxamide


InChi Code: InChI=1S/C32H44N4O4/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/h7-8,11-12,14,18,22-23,26,28H,3-6,9-10,13,15-17,19-21H2,1-2H3,(H,34,38)(H,35,37)/t22-,26-,28-/m0/s1

SMILES Code: O=C(C1=CC=NO1)N[C@@H](CC2CCCCC2)C(N[C@@H]([C@@H](C)CC)C(N3CCC4(CC3)CCC5=C4C=CC=C5)=O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 548.73 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Muley MM, Krustev E, Reid AR, McDougall JJ. Prophylactic inhibition of neutrophil elastase prevents the development of chronic neuropathic pain in osteoarthritic mice. J Neuroinflammation. 2017 Aug 23;14(1):168. doi: 10.1186/s12974-017-0944-0. PubMed PMID: 28835277; PubMed Central PMCID: PMC5569523.

2: Ostertag D, Annahazi A, Krueger D, Michel K, Demir IE, Ceyhan GO, Zeller F, Schemann M. Tryptase potentiates enteric nerve activation by histamine and serotonin: Relevance for the effects of mucosal biopsy supernatants from irritable bowel syndrome patients. Neurogastroenterol Motil. 2017 Sep;29(9). doi: 10.1111/nmo.13070. Epub 2017 Apr 4. PubMed PMID: 28374503.

3: Indrakusuma I, Romacho T, Eckel J. Protease-Activated Receptor 2 Promotes Pro-Atherogenic Effects through Transactivation of the VEGF Receptor 2 in Human Vascular Smooth Muscle Cells. Front Pharmacol. 2017 Jan 4;7:497. doi: 10.3389/fphar.2016.00497. eCollection 2016. PubMed PMID: 28101054; PubMed Central PMCID: PMC5209375.

4: Cho NC, Seo SH, Kim D, Shin JS, Ju J, Seong J, Seo SH, Lee I, Lee KT, Kim YK, No KT, Pae AN. Pharmacophore-based virtual screening, biological evaluation and binding mode analysis of a novel protease-activated receptor 2 antagonist. J Comput Aided Mol Des. 2016 Aug;30(8):625-37. doi: 10.1007/s10822-016-9937-9. Epub 2016 Sep 6. PubMed PMID: 27600555.

5: Romacho T, Vallejo S, Villalobos LA, Wronkowitz N, Indrakusuma I, Sell H, Eckel J, Sánchez-Ferrer CF, Peiró C. Soluble dipeptidyl peptidase-4 induces microvascular endothelial dysfunction through proteinase-activated receptor-2 and thromboxane A2 release. J Hypertens. 2016 May;34(5):869-76. doi: 10.1097/HJH.0000000000000886. PubMed PMID: 26895560.

6: Muley MM, Reid AR, Botz B, Bölcskei K, Helyes Z, McDougall JJ. 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. Epub 2015 Jul 31. PubMed PMID: 26140667; PubMed Central PMCID: PMC4742294.

7: Bukowska A, Zacharias I, Weinert S, Skopp K, Hartmann C, Huth C, Goette A. Coagulation factor Xa induces an inflammatory signalling by activation of protease-activated receptors in human atrial tissue. Eur J Pharmacol. 2013 Oct 15;718(1-3):114-23. doi: 10.1016/j.ejphar.2013.09.006. Epub 2013 Sep 13. PubMed PMID: 24041930.

8: Barry GD, Suen JY, Le GT, Cotterell A, Reid RC, Fairlie DP. Novel agonists and antagonists for human protease activated receptor 2. J Med Chem. 2010 Oct 28;53(20):7428-40. doi: 10.1021/jm100984y. PubMed PMID: 20873792.