1234510-46-3
Chemical Structure
TRV-120027
Synonym(s): TRV027
- CAS No.: 1234510-46-3
- Formula:C43H67N13O10
- Molecular Weight:926.07
InChIKey: XIEWFECSPPTVQN-KMIMAYJXSA-N
SMILES: C[C@H](C(O)=O)NC([C@H]1N(C([C@H](CC2=CNC=N2)NC([C@H]([C@@H](C)CC)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
Biological Activity: TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages β-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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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TRV-120027 | 98.21% | TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages β-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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- [1]. 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. [Content Brief]
- [2]. Liu CH, et al. Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling.Nat Commun. 2017 Feb 9;8:14335. [Content Brief]
Keywords
