TRV-120027 is an investigational drug designed as a selective, orally bioavailable, small molecule that inhibits the activity of the TRPC5 ion channel.
CAT No: R1867
CAS No:1234510-46-3
Synonyms/Alias:TRV-120027;1234510-46-3;trv027;TRV120027;TRV-027;UNII-J1J4P3PQZD;TRV 027;J1J4P3PQZD;TRV 120027;D-Alanine, N-methylglycyl-L-arginyl-L-valyl-L-tyrosyl-L-isoleucyl-L-histidyl-L-prolyl-;Sar-val-tyr-ile-his-pro-d-ala-oh;(2R)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]propanoic acid;Sar-Arg-Val-Tyr-Ile-His-Pro-Ala;GTPL6902;CHEMBL4297447;TRV 027 [WHO-DD];GLXC-27746;HY-P2141;AKOS040764215;DB12199;NMeGly-Arg-Val-Tyr-Ile-His-Pro-DAla;DA-58776;CS-0109050;NS00073768;G17966;Q27281029;
Chemical Name:(2R)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]propanoic acid
TRV-120027 is a synthetic peptide compound designed to modulate specific G protein-coupled receptor (GPCR) signaling pathways, particularly within the context of cardiovascular and pharmacological research. As a biased ligand for the angiotensin II type 1 receptor (AT1R), TRV-120027 exhibits unique signaling properties that distinguish it from conventional agonists or antagonists. Its ability to selectively engage beta-arrestin-mediated pathways while minimizing G protein activation has positioned it as a valuable tool for dissecting the mechanistic nuances of receptor signaling bias. Researchers utilize this compound to explore novel paradigms in receptor pharmacology and to investigate the physiological consequences of pathway-selective modulation.
Receptor Signaling Studies: TRV-120027 serves as a critical probe for elucidating the mechanisms of biased agonism at the AT1R. By preferentially activating beta-arrestin pathways over classical G protein-mediated responses, it allows researchers to dissect the distinct downstream effects associated with each signaling route. This selective engagement provides deeper insight into the functional selectivity of GPCRs, advancing understanding of receptor conformational dynamics and the molecular basis of biased signaling.
Cardiovascular Research: The compound is widely employed in studies investigating the role of AT1R signaling in cardiovascular physiology and pathophysiology. Its unique signaling profile enables the assessment of beta-arrestin-dependent effects on cardiac contractility, vascular tone, and remodeling processes. By differentiating between G protein and beta-arrestin-mediated outcomes, investigators can clarify the contributions of each pathway to cardiovascular homeostasis and disease mechanisms, supporting the development of more targeted research models.
Pharmacological Profiling: TRV-120027 is instrumental in high-content screening and pharmacological profiling of GPCR-targeted compounds. Its use as a reference ligand helps to benchmark the signaling bias of new molecular entities, facilitating the identification and characterization of novel biased agonists or antagonists. This application is particularly valuable in drug discovery contexts, where understanding the signaling landscape of candidate molecules can inform structure-activity relationships and guide lead optimization.
Peptide Structure-Activity Relationship (SAR) Analysis: The synthetic peptide nature of TRV-120027 makes it suitable for detailed SAR studies aimed at correlating specific sequence modifications with functional outcomes. Researchers employ the compound to investigate how alterations in peptide structure influence receptor selectivity, efficacy, and signaling bias. These insights are essential for the rational design of next-generation peptide ligands with tailored pharmacological properties.
In vitro Assay Development: Owing to its well-characterized signaling behavior, TRV-120027 is frequently used as a control or reference compound in the development and validation of in vitro assays targeting AT1R or related GPCRs. Its predictable engagement of beta-arrestin pathways provides a reliable benchmark for assay sensitivity and specificity, ensuring robust experimental design for both academic and industrial research settings. This application supports the generation of reproducible data and the advancement of innovative screening platforms.
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