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TRV-120027 TFA

Catalog No. TP2158   CAS TP2158
Synonyms: TRV-120027 TFA (1234510-46-3 free base)

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.

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TRV-120027 TFA Chemical Structure
TRV-120027 TFA, CAS TP2158
Pack Size Availability Price/USD Quantity
1 mg In stock $ 64.00
5 mg In stock $ 198.00
10 mg In stock $ 315.00
25 mg In stock $ 542.00
50 mg In stock $ 782.00
100 mg In stock $ 1,070.00
1 mL * 10 mM (in DMSO) In stock $ 359.00
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Purity: 97.45%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 the angiotensin II receptor type 1:
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].
Synonyms TRV-120027 TFA (1234510-46-3 free base)
Molecular Weight 1040.1
Formula C45H68F3N13O12
CAS No. TP2158

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 88 mg/mL (84.61 mM)

TargetMolReferences and Literature

1. Liu CH, et al. Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling.Nat Commun. 2017 Feb 9;8:14335. 2. Boerrigter G, et al. TRV120027, a novel β-arrestin biased ligand at the angiotensin II type I receptor, unloads the heart and maintains renal function when added to furosemide in experimental heart failure.Circ Heart Fail. 2012 Sep 1;5(5):627-34. Epub 2012 Aug 13.

Related compound libraries

This product is contained In the following compound libraries:
Peptide Compound Library Inhibitor Library Anti-Hypertension Compound Library Clinical Compound Library Endocrinology-Hormone Compound Library Bioactive Compounds Library Max Anti-Cardiovascular Disease Compound Library Bioactive Compound Library Drug Repurposing Compound Library

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Keywords

TRV-120027 TFA TP2158 Endocrinology/Hormones GPCR/G Protein RAAS Arrestin 1234510-46-3 TRV 120027 TFA 1234510-46-3 free base TRV120027 TFA TRV-120027 TFA (1234510-46-3 free base) inhibitor inhibit

 

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