| Name | TRV-120027 TFA |
| Description | TRV-120027 TFA is an angiotensin II–mediated vasoconstriction inhibitor and increases cardiomyocyte contractility. TRV-120027 TFA is a β-arrestin-1-biased AT1R agonist engaging ß-arrestins while blocking G-protein signaling[1]. TRV-120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling and promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. |
| In vitro | Treatment of 100 nM TRV-120027 TFA 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[1]. Treatment of 100 nM TRV-120027 TFA significantly increases the AT1R and TRPC3 association with the immunoprecipitated β-arrestin-1 in HEK293 cells co-transfected with Flag-AT1R-cherry, HA-β-arrestin-1 and TRPC3-GFP[1]. |
| In vivo | TRV-120027 TFA combined with furosemide decreases cardiac preload and afterload, systemic and renal vascular resistances, and left ventricular external work while increasing cardiac output and renal blood flow[2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (3.17 mM), Sonication is recommended.
DMSO : 88 mg/mL (84.61 mM), Sonication is recommended.
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| Keywords | TRV-120027 TFA | TRV120027 TFA | TRV 120027 TFA | TRPVChannel | TRPV Channel | TRPChannel | TRP Channel | the angiotensin II receptor type 1 | AT1 receptor | 1234510-46-3 free base | 1234510-46-3 |
| Inhibitors Related | Losartan potassium | Rosiglitazone | Caffeic Acid | Tranilast | Probenecid | Sacubitril/Valsartan | 1,4-Cineole | Benzyl benzoate | trans-Cinnamaldehyde | Losartan | Diisononyl phthalate | Captopril |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Peptide Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Ion Channel Targeted Library | GPCR Compound Library | Anti-Hypertension Compound Library |
United States
