1. GPCR/G Protein
  2. Angiotensin Receptor
  3. TRV-120027 TFA

TRV-120027 TFA 

Cat. No.: HY-P2141A Purity: 99.21%
Handling Instructions

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

For research use only. We do not sell to patients.

Custom Peptide Synthesis

TRV-120027 TFA Chemical Structure

TRV-120027 TFA Chemical Structure

Size Price Stock Quantity
1 mg USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Description

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].

IC50 & Target

IC50: the angiotensin II receptor type 1 (AT1R)[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TRV120027 TFA (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male mongrel dogs (weight, 20.5–30 kg)[1]
Dosage: 0.3 or 1.5 µg/kg per minute; infusion rate, 0.5 mL/min
Administration: Intravenous injection
Result: Resulted in dose-dependent vasodilation, increased cardiac contractility, and decreased myocardial oxygen consumption in dog.
Clinical Trial
Molecular Weight

1040.10

Formula

C₄₅H₆₈F₃N₁₃O₁₂

Sequence

{Sar}-Arg-Val-Tyr-Ile-His-Pro-Ala

Sequence Shortening

{Sar}-RVYIHPA

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Protect from light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

References
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Keywords:

TRV-120027TRV120027TRV 120027Angiotensin ReceptoracutedecompensatedheartfailureADHFAT1RInhibitorinhibitorinhibit

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TRV-120027 TFA
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