| Bioactivity | TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-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]. | ||||||
| Invitro | 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, HA-β-arrestin-1 and TRPC3-GFP[2].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[2]. | ||||||
| Name | TRV-120027 TFA | ||||||
| Sequence | {Sar}-Arg-Val-Tyr-Ile-His-Pro-Ala | ||||||
| Shortening | {Sar}-RVYIHPA | ||||||
| Formula | C45H68F3N13O12 | ||||||
| Molar Mass | 1040.10 | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | Sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
TRV-120027 TFA
CAS: F: C45H68F3N13O12 W: 1040.10
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while b
Data collection：peptidedb@qq.com
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