Page last updated: 2024-12-07

cgp 42112a

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

CGP 42112A: a hexapeptide analog of angiotensin II; activation of Receptor, Angiotensin, Type 2 results in vasodilation [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

CGP-42112A : A hexapeptide consisting of L-tyrosine, L-lysine, L-histidine, L-proline and L-isoleucine amino acid residues coupled in sequence and in which the amino group of the L-tyrosyl residue is substituted by a (pyridin-3-ylcarbonyl)nitrilo group and in which the L-lysyl side chain amino group is substituted by a {N(2)-[(benzyloxy)carbonyl]-L-arginyl}nitrilo group. It is a potent angiotensin II receptor type 2 (AT2 receptor) agonist. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID123794
CHEMBL ID1885579
CHEBI ID147302
SCHEMBL ID15524960
SCHEMBL ID16675400
MeSH IDM0168978

Synonyms (46)

Synonym
gtpl594
[125i]-cgp42112
[125i]cgp42112
(2s,3s)-2-[[(2s)-1-[(2s)-2-[[(2s)-6-[[(2s)-5-(diaminomethylideneamino)-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-2-[[(2s)-3-(4-hydroxyphenyl)-2-(pyridine-3-carbonylamino)propanoyl]amino]hexanoyl]amino]-3-(3h-imidazol-4-yl)propanoyl]pyrrolidine-2-carb
PDSP1_000402
PDSP2_000400
cgp42112a
cgp-42112a, >=95%, synthetic, solid
nicotinic acid-tyrosyl-(n(sigma)-benzyloxycarbonyl-arginyl)lysyl-histidyl-prolyl-isoleucine-oh
nicotinic acid-tyr-(n(sigma)-benzyloxycarbonyl-arg)lys-his-pro-ile-oh
cgp 42112
l-isoleucine, n-(1-(n-(n6-(n2-((phenylmethoxy)carbonyl)-l-arginyl)-n2-(n-(3-pyridinylcarbonyl)-l-tyrosyl)-l-lysyl)-l-histidyl)-l-prolyl)-
cgp 42112b
cgp-42112a
cgp 42112a
NCGC00167317-01
127060-75-7
cgp42112
cgp-42112
(2s,3s)-2-[[(2s)-1-[(2s)-2-[[(2s)-6-[[(2s)-5-(diaminomethylideneamino)-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-2-[[(2s)-3-(4-hydroxyphenyl)-2-(pyridine-3-carbonylamino)propanoyl]amino]hexanoyl]amino]-3-(1h-imidazol-5-yl)propanoyl]pyrrolidine-2-carb
n(6)-{n(2)-[(benzyloxy)carbonyl]-l-arginyl}-n(2)-[n-(pyridine-3-carbonyl)-l-tyrosyl]-l-lysyl-l-histidyl-l-prolyl-l-isoleucine
n(6)-{n(2)-[(benzyloxy)carbonyl]-l-arginyl}-n(2)-[n-(pyridin-3-ylcarbonyl)-l-tyrosyl]-l-lysyl-l-histidyl-l-prolyl-l-isoleucine
n(6)-[[(phenylmethoxy)carbonyl]-l-arg-]-n(2)-[[(pyridin-3-yl)carbonyl]-l-tyr-]-l-lys-l-his-l-pro-l-ile-oh
nalpha-nicotinoyl-tyr-(nalpha-cbz-arg)-lys-his-pro-ile
CHEBI:147302
unii-9q3v7w3xdd
9q3v7w3xdd ,
gtpl3944
CS-3414
SCHEMBL15524960
CHEMBL1885579 ,
HY-12405
AKOS024457173
mfcd00133611
DTXSID90155396
SCHEMBL16675400
angiotensin ii receptor ligand (nicotinoyl-tyr-lys(1)-his-pro-ile-oh.cbz-arg-(1))
BS-15127
Q27075903
l-isoleucine, n-(3-pyridinylcarbonyl)-l-tyrosyl-n6-(n2-((phenylmethoxy)carbonyl)-l-arginyl)-l-lysyl-l-histidyl-l-prolyl-
n-(3-pyridinylcarbonyl)-l-tyrosyl-n6-(n2-((phenylmethoxy)carbonyl)-l-arginyl)-l-lysyl-l-histidyl-l-prolyl-l-isoleucine
EX-A7392
D83656
n6-(((benzyloxy)carbonyl)-l-arginyl)-n2-(nicotinoyl-l-tyrosyl)-l-lysyl-l-histidyl-l-prolyl-l-isoleucine
AKOS037648666
bdbm50514581

Research Excerpts

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
angiotensin receptor agonistA hormone antagonist that acts at angiotensin receptors.
vasodilator agentA drug used to cause dilation of the blood vessels.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
anti-inflammatory agentAny compound that has anti-inflammatory effects.
neuroprotective agentAny compound that can be used for the treatment of neurodegenerative disorders.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
oligopeptideA peptide containing a relatively small number of amino acids.
benzyl ester
pyridinecarboxamideA member of the class of pyridines that is a substituted pyridine in which at least one of the substituents is a carboxamide or N-substituted caraboxamide group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (1)

PathwayProteinsCompounds
Renin-angiotensin pathway (COVID-19 Disease Map)116

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA polymerase kappa isoform 1Homo sapiens (human)Potency15.00300.031622.3146100.0000AID588579
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)Ki1.70000.00020.10251.7000AID1560687
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID1346340Human AT2 receptor (Angiotensin receptors)1991Biochemical and biophysical research communications, Dec-31, Volume: 181, Issue:3
Radioiodinated CGP 42112A: a novel high affinity and highly selective ligand for the characterization of angiotensin AT2 receptors.
AID1346340Human AT2 receptor (Angiotensin receptors)1989Biochemical and biophysical research communications, Aug-30, Volume: 163, Issue:1
Preliminary biochemical characterization of two angiotensin II receptor subtypes.
AID1346340Human AT2 receptor (Angiotensin receptors)2011Clinical science (London, England : 1979), Oct, Volume: 121, Issue:7
Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors.
AID1560687Displacement of [125I]Ang II from AT1 receptor in rat SMC membranes incubated for 60 mins by gamma counting method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
The Other Angiotensin II Receptor: AT
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (228)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.44)18.7374
1990's126 (55.26)18.2507
2000's64 (28.07)29.6817
2010's34 (14.91)24.3611
2020's3 (1.32)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.64

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index16.64 (24.57)
Research Supply Index5.46 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.64)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews5 (2.15%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other228 (97.85%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]