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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $38 | In Stock | |
5 mg | $119 | In Stock | |
10 mg | $189 | In Stock | |
25 mg | $325 | In Stock | |
50 mg | $469 | In Stock | |
100 mg | $642 | In Stock | |
200 mg | $865 | In Stock | |
1 mL x 10 mM (in DMSO) | $215 | In Stock |
Description | TRV120027 TFA is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R) and engages ß-arrestins while blocking G-protein signaling. |
Targets&IC50 | Ang II type 1 receptor: |
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]. |
Alias | TRV-120027 TFA (1234510-46-3 free base) |
Molecular Weight | 1040.1 |
Formula | C45H68F3N13O12 |
Smiles | O=C(O)C(F)(F)F.C[C@H](C(O)=O)NC([C@H]1N(C([C@H](CC2=CNC=N2)NC([C@]([C@H](C)CC)([H])NC([C@@H](CC3=CC=C(O)C=C3)NC([C@H](C(C)C)NC([C@H](CCCNC(N)=N)NC(CNC)=O)=O)=O)=O)=O)=O)CCC1)=O |
Relative Density. | 1.31g/cm3 |
Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 88 mg/mL (84.61 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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