TRV-120027 (TFA)

TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages β-arrestins while blocking G-protein signaling[1]. TRV120027 TFA 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 TFA inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment[2].

Product Specifications

UNSPSC

12352209

Target

Angiotensin Receptor; Arrestin

Type

Peptides

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

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

Purity

99.69

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

OC(C(F)(F)F)=O.CC[C@@H]([C@@H](C(N[C@H](C(N1CCC[C@H]1C(N[C@@H](C(O)=O)C)=O)=O)CC2=CNC=N2)=O)NC([C@@H](NC([C@H](C(C)C)NC([C@@H](NC(CNC)=O)CCCNC(N)=N)=O)=O)CC3=CC=C(O)C=C3)=O)C

Molecular Formula

C45H68F3N13O12

Molecular Weight

1040.10

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.

Shipping Conditions

Blue Ice

Storage Conditions

-80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture and light)

Scientific Category

Peptides

Clinical Information

Phase 2

Isoform

AT1 Receptor

Citation 01

J Am Heart Assoc. 2022 Feb 15;11 (4) :e022070.|University of Medicine Berlin. 2023 Mar.|Eur J Pharmacol. 2023 Jul 15:951:175780.

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