Synonyms: 3-[4-(1H-imidazol-1-ylmethyl)phenyl]-5-(2-methylpropyl)thiophene-2-[(N-butyloxylcarbamate)-sulphonamide] sodium salt | C21
Compound class:
Synthetic organic
Comment: Compound 21 is a first-in-class orally administered angiotensin AT2 receptor agonist. It prevents TNFα-induced and HFD-induced vascular inflammation in vitro and in vivo, indicating that its anti-atherosclerotic actions are due to vascular anti-inflammatory effects, mediated by AT2 receptors [2]. C21 is one of the chemical structures that are claimed in Vicore Pharma's patent US20180078529A1 [1].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Dahlof B, Ljunggren A. (2018)
Angiotensin ii receptor agonist for treating pulmonary fibrosis. Patent number: US20180078529A1. Assignee: Vicore Pharma AB. Priority date: 03/02/2015. Publication date: 22/03/2018. |
2. Sampson AK, Irvine JC, Shihata WA, Dragoljevic D, Lumsden N, Huet O, Barnes T, Unger T, Steckelings UM, Jennings GL et al.. (2016)
Compound 21, a selective agonist of angiotensin AT2 receptors, prevents endothelial inflammation and leukocyte adhesion in vitro and in vivo. Br J Pharmacol, 173 (4): 729-40. [PMID:25560767] |
3. Tornling G, Batta R, Porter JC, Williams B, Bengtsson T, Parmar K, Kashiva R, Hallberg A, Cohrt AK, Westergaard K et al.. (2021)
Seven days treatment with the angiotensin II type 2 receptor agonist C21 in hospitalized COVID-19 patients; a placebo-controlled randomised multi-centre double-blind phase 2 trial. EClinicalMedicine, 41: 101152. [PMID:34723163] |
4. Verdonk K, Durik M, Abd-Alla N, Batenburg WW, van den Bogaerdt AJ, van Veghel R, Roks AJ, Danser AH, van Esch JH. (2012)
Compound 21 induces vasorelaxation via an endothelium- and angiotensin II type 2 receptor-independent mechanism. Hypertension, 60 (3): 722-9. [PMID:22802221] |
5. Wan Y, Wallinder C, Plouffe B, Beaudry H, Mahalingam AK, Wu X, Johansson B, Holm M, Botoros M, Karlén A et al.. (2004)
Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist. J Med Chem, 47 (24): 5995-6008. [PMID:15537354] |