TRV-120027 acetate is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1 receptor) and engages -arrestins while blocking G-protein signaling.

TRV120027 TFA (100 nM) induces an [Ca2+]i increase in HEK293 cells co-transfected with AT1R, β-arrestin-1, and TRPC3, which are significantly blocked by Pyr3 pre-incubation in HEK293 cells co-transfected with Flag-AT1R-Cherry, HA-β-arrestin-1, and TRPC3-GFP. TRV120027 TFA (100 nM) significantly increases the AT1R and TRPC3 association with the immunoprecipitated β-arrestin-1 in HEK293 cells co-transfected with Flag-AT1R-cherry, TRPC3-GFP, and HA-β-arrestin-1 [2].

TRV120027 TFA (i.v.; 0.3 or 1.5 μg/kg per minute; infusion rate, 0.5 mL/min), when added to furosemide, decreases cardiac preload and afterload, systemic and renal vascular resistance, and left ventricular external work while increasing cardiac output and renal blood flow [1].