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MedChemExpress - Model TRV-120027 -1234510-46-3

TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-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].

TRV-120027

MCE China：TRV-120027

Brand：MedChemExpress (MCE)

Cat. No.HY-P2141

CAS：1234510-46-3

Purity：98.11%

Storage：Sealed storage, away from moisture and light, under nitrogen Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling. 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.

In Vitro：TRV120027 (100 nM) 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[2]. TRV120027 (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[2].

In Vivo：TRV120027 (intravenous?injection; 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 resistances, and left ventricular external work while increasing cardiac output and renal blood flow. GFR and renal excretory function are maintained in canines with experimental HF[1].

IC50 & Target：AT1 Receptor

References：

[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. [Content Brief]

[2]. Liu CH, et al. Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling.Nat Commun. 2017 Feb 9;8:14335. [Content Brief]

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MedChemExpress - Model TRV-120027 -1234510-46-3

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TRV-120027