CGP-42112A is a potent angiotensin II receptor type 2 (AT2 receptor) agonist. It has a role as an angiotensin receptor agonist, a vasodilator agent, an antineoplastic agent, an anti-inflammatory agent and a neuroprotective agent.
CAT No: R1850
CAS No:127060-75-7
Synonyms/Alias:127060-75-7;Cgp 42112;Cgp-42112A;CGP-42112;CGP 42112A;Cgp 42112B;CGP42112A;CGP42112;MFCD00133611;9Q3V7W3XDD;CHEMBL1885579;L-Isoleucine, N-(1-(N-(N6-(N2-((phenylmethoxy)carbonyl)-L-arginyl)-N2-(N-(3-pyridinylcarbonyl)-L-tyrosyl)-L-lysyl)-L-histidyl)-L-prolyl)-;Nalpha-Nicotinoyl-Tyr-(Nalpha-Cbz-Arg)-Lys-His-Pro-Ile;(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-carbonyl]amino]-3-methylpentanoic acid;Nicotinic acid-tyr-(N(sigma)-benzyloxycarbonyl-arg)lys-his-pro-ile-OH;N6-(((benzyloxy)carbonyl)-L-arginyl)-N2-(nicotinoyl-L-tyrosyl)-L-lysyl-L-histidyl-L-prolyl-L-isoleucine;(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-carbonyl]amino]-3-methylpentanoic acid;Nicotinic acid-tyrosyl-(N(sigma)-benzyloxycarbonyl-arginyl)lysyl-histidyl-prolyl-isoleucine-OH;[125I]CGP42112;[125I]-CGP42112;AngiotensinIIReceptorLigand;UNII-9Q3V7W3XDD;GTPL594;GTPL3944;SCHEMBL15524960;SCHEMBL16675400;DTXSID90155396;CHEBI:147302;EX-A7392;BDBM50514581;PDSP1_000402;PDSP2_000400;AKOS024457173;AKOS037648666;CGP-42112?;CS-3414;NCGC00167317-01;BS-15127;FA110425;HY-12405;CGP-42112A, >=95%, synthetic, solid;D83656;Q27075903;Angiotensin II Receptor Ligand Nicotinoyl-Tyr-Lys(Z-Arg)-His-Pro-Ile-OH;Angiotensin II Receptor Ligand (Nicotinoyl-Tyr-Lys(1)-His-Pro-Ile-OH.CbZ-Arg-(1));(2S,3S)-2-((S)-1-((5S,12S,15S)-15-((1H-Imidazol-5-yl)methyl)-5-(3-guanidinopropyl)-12-((S)-3-(4-hydroxyphenyl)-2-(nicotinamido)propanamido)-3,6,13-trioxo-1-phenyl-2-oxa-4,7,14-triazahexadecan-16-oyl)pyrrolidine-2-carboxamido)-3-methylpentanoic acid;(2S,3S)-2-{[(2S)-1-[(2S)-2-[(2S)-6-[(2S)-2-{[(BENZYLOXY)CARBONYL]AMINO}-5-CARBAMIMIDAMIDOPENTANAMIDO]-2-[(2S)-3-(4-HYDROXYPHENYL)-2-(PYRIDIN-3-YLFORMAMIDO)PROPANAMIDO]HEXANAMIDO]-3-(1H-IMIDAZOL-4-YL)PROPANOYL]PYRROLIDIN-2-YL]FORMAMIDO}-3-METHYLPENTANOIC ACID;L-ISOLEUCINE, N-(3-PYRIDINYLCARBONYL)-L-TYROSYL-N6-(N2-((PHENYLMETHOXY)CARBONYL)-L-ARGINYL)-L-LYSYL-L-HISTIDYL-L-PROLYL-;N(6)-[[(phenylmethoxy)carbonyl]-L-Arg-]-N(2)-[[(pyridin-3-yl)carbonyl]-L-Tyr-]-L-Lys-L-His-L-Pro-L-Ile-OH;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)-{N(2)-[(benzyloxy)carbonyl]-L-arginyl}-N(2)-[N-(pyridine-3-carbonyl)-L-tyrosyl]-L-lysyl-L-histidyl-L-prolyl-L-isoleucine;N-(3-PYRIDINYLCARBONYL)-L-TYROSYL-N6-(N2-((PHENYLMETHOXY)CARBONYL)-L-ARGINYL)-L-LYSYL-L-HISTIDYL-L-PROLYL-L-ISOLEUCINE;
Chemical Name:N6-(((benzyloxy)carbonyl)-L-arginyl)-N2-(nicotinoyl-L-tyrosyl)-L-lysyl-L-histidyl-L-prolyl-L-isoleucine
CGP-42112A is a synthetic peptide compound that functions as a selective angiotensin II type 2 receptor (AT2R) agonist, making it a valuable tool for investigating the renin-angiotensin system and its diverse physiological roles. Structurally designed to mimic specific angiotensin II motifs, this peptide enables researchers to probe the distinct signaling pathways and biological outcomes associated with AT2R activation, independent of type 1 receptor (AT1R) effects. Its selectivity and stability have positioned it as a central molecule in studies dissecting the complex interplay between peptide hormones, receptor subtypes, and downstream cellular responses in cardiovascular, renal, and neurobiological contexts.
Receptor pharmacology: As a highly selective AT2R agonist, CGP-42112A is extensively utilized in receptor binding and signal transduction studies to delineate the functional roles of AT2R in comparison to AT1R. By enabling precise activation of AT2R, it supports the characterization of receptor-specific signaling cascades, including those involving nitric oxide synthesis, phosphatase activity, and cyclic GMP modulation. This specificity is critical for researchers seeking to unravel the molecular mechanisms underlying angiotensin II-mediated effects in various cell types and tissues.
Cardiovascular research: The compound is widely employed in cardiovascular physiology experiments to explore the protective and regulatory functions of AT2R in blood vessels and cardiac tissue. Investigations using this peptide have advanced understanding of vasodilation, anti-proliferative effects on vascular smooth muscle cells, and the attenuation of hypertrophic responses. Its application allows for the isolation of AT2R-mediated pathways, providing insight into the receptor's potential role in counterbalancing the pressor and remodeling actions typically attributed to AT1R stimulation.
Renal function studies: CGP-42112A serves as a critical reagent in nephrology research, particularly in the context of renal hemodynamics and sodium handling. By selectively engaging AT2R, it facilitates the examination of natriuretic mechanisms, glomerular filtration dynamics, and the modulation of renal vascular tone. Utilization of this peptide in experimental models has contributed to a deeper comprehension of how AT2R activation may influence renal protective processes and fluid-electrolyte balance.
Neurobiological investigations: In neuroscience, this peptide is applied to assess the involvement of AT2R in neuronal differentiation, neuroprotection, and synaptic plasticity. Its use in in vitro and in vivo models enables the dissection of angiotensinergic signaling within the central and peripheral nervous systems, with particular emphasis on neuronal growth, apoptosis regulation, and the modulation of neurotransmitter release. These studies are pivotal for mapping the broader physiological relevance of AT2R beyond traditional cardiovascular and renal frameworks.
Peptide signaling research: Owing to its synthetic peptide nature and receptor selectivity, CGP-42112A is an essential tool in peptide signaling research. It provides a model for studying structure-activity relationships among angiotensin-derived peptides and their interactions with G protein-coupled receptors. Researchers leverage this compound to develop and validate new analytical methods, optimize receptor-ligand binding assays, and explore the design of next-generation peptide agonists with tailored pharmacological profiles. Its applications thus extend to both fundamental receptor biology and the advancement of peptide-based research methodologies.
3. Adipose tissue is a key organ for the beneficial effects of GLP-2 metabolic function
5. High fat diet and GLP-1 drugs induce pancreatic injury in mice
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