2. GPCR/G Protein
  3. Angiotensin Receptor Arrestin
  4. TRV-120027

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 the acute decompensated heart failure (ADHF) treatment.

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TRV-120027 Chemical Structure

TRV-120027 Chemical Structure

CAS No. : 1234510-46-3

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Based on 3 publication(s) in Google Scholar

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TRV-120027 Related Antibodies

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Description

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

IC50 & Target

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

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

TRV-120027 Related Antibodies
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].

MedChemExpress (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

926.07

Formula

C43H67N13O10
CAS No.
Appearance

Solid

Color

White to off-white

Sequence Shortening

{Sar}-RVYIHPA
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (107.98 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0798 mL 5.3992 mL 10.7983 mL
5 mM 0.2160 mL 1.0798 mL 2.1597 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.0798 mL 5.3992 mL 10.7983 mL 26.9958 mL
5 mM 0.2160 mL 1.0798 mL 2.1597 mL 5.3992 mL
10 mM 0.1080 mL 0.5399 mL 1.0798 mL 2.6996 mL
15 mM 0.0720 mL 0.3599 mL 0.7199 mL 1.7997 mL
20 mM 0.0540 mL 0.2700 mL 0.5399 mL 1.3498 mL
25 mM 0.0432 mL 0.2160 mL 0.4319 mL 1.0798 mL
30 mM 0.0360 mL 0.1800 mL 0.3599 mL 0.8999 mL
40 mM 0.0270 mL 0.1350 mL 0.2700 mL 0.6749 mL
50 mM 0.0216 mL 0.1080 mL 0.2160 mL 0.5399 mL
60 mM 0.0180 mL 0.0900 mL 0.1800 mL 0.4499 mL
80 mM 0.0135 mL 0.0675 mL 0.1350 mL 0.3374 mL
100 mM 0.0108 mL 0.0540 mL 0.1080 mL 0.2700 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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TRV-120027 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TRV-1200271234510-46-3TRV120027TRV 120027Angiotensin ReceptorArrestinAT1R?acutedecompensatedheartfailureADHF cardiacInhibitorinhibitorinhibit

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