TRV-120027

TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages β-arrestins while blocking G-protein signaling[1]. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R-β-arrestin-1-TRPC3-PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment[2].

Product Specifications

CAS Number

[1234510-46-3]

Product Name Alternative

TRV027

UNSPSC

12352209

Target

Angiotensin Receptor; Arrestin

Type

Peptides

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/trv-120027.html

Purity

98.11

Solubility

H2O : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

C[C@H](C(O)=O)NC([C@H]1N(C([C@H](CC2=CNC=N2)NC([C@H]([C@@H](C)CC)NC([C@H](CC3=CC=C(O)C=C3)NC([C@H](C(C)C)NC([C@H](CCCNC(N)=N)NC(CNC)=O)=O)=O)=O)=O)=O)CCC1)=O

Molecular Formula

C43H67N13O10

Molecular Weight

926.07

References & Citations

[1]Boerrigter G, et al. TRV120027, a novel β-arrestin biased ligand at the angiotensin II type I receptor, unloads the heart and maintains renal function when added to furosemide in experimental heart failure.Circ Heart Fail. 2012 Sep 1;5 (5) :627-34. Epub 2012 Aug 13.|[2]Liu CH, et al. Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling.Nat Commun. 2017 Feb 9;8:14335.