TargetMol

TRV-120027 TFA

Product Code:
 
TAR-TP2158
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
 

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CodeSizePrice
TAR-TP2158-1mg1mg£122.00
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TAR-TP2158-5mg5mg£230.00
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TAR-TP2158-10mg10mg£324.00
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TAR-TP2158-1mL1 mL * 10 mM (in DMSO)£359.00
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TAR-TP2158-25mg25mg£506.00
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TAR-TP2158-50mg50mg£699.00
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TAR-TP2158-100mg100mg£930.00
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Further Information

Bioactivity:
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 ?-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.
CAS:
TP2158
Formula:
C45H68F3N13O12
Molecular Weight:
1040.1
Pathway:
Endocrinology/Hormones
Purity:
0.9745
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
Target:
RAAS

References

Boerrigter G, et al. TRV120027, a novel ?-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. Liu CH, et al. Arrestin-biased?AT1R?agonism?induces?acute?catecholamine?secretion?through?TRPC3?coupling.Nat Commun.?2017 Feb 9;8:14335.