TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-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 acute decompensated heart failure (ADHF) treatment.
CAT# | R1867 |
CAS | 1234510-46-3 |
Chemical Name | (2R)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]propanoic acid |
M.F/Formula | C43H67N13O10 |
M.W/Mr. | 926.1 |
Sequence | One Letter Code: Sar-RVYIHPA Three Letter Code: H-Sar-Arg-Val-Tyr-Ile-His-Pro-D-Ala-OH |
Application | TRV120027 has been used in trials studying the treatment of Heart Failure and Kidney Disease. |
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