GB83

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MedKoo CAT#: 527107

CAS#: 1252806-86-2

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


Price and Availability

Size Price Shipping out time Quantity
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Pricing updated 2020-04-01. Prices are subject to change without notice.

GB83 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 527107
Name: GB83
CAS#: 1252806-86-2
Chemical Formula: C32H44N4O4
Exact Mass: 548.3363
Molecular Weight: 548.728
Elemental Analysis: C, 70.04; H, 8.08; N, 10.21; O, 11.66


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 Key: ZXMXAOYWSLZLQM-MCOVPRHSSA-N

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


Technical Data

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


References

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.