VTP 27999 trifluoroacetate
Chemical Name: Methyl N-[2-[(R)-(3-Chlorophenyl)[(3R)-1-[[[(2S)-2-(methylamino)-3-[(3R)-tetrahydro-2H-pyran-3-yl]propyl]amino]carbonyl]-3-piperidinyl]methoxy]ethyl]carbamate trifluoroacetate
Biological ActivityVTP 27999 trifluoroacetate is a highly potent and selective renin inhibitor (IC50 = 0.47 nM). Displays >1000-fold selectivity over related and unrelated off-targets. Blocks renin-stimulated ERK1/2 phosphorylation in vascular smooth muscle cells. Exhibits a different mode of action to aliskiren (Cat. No. 5491).
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of VTP-27999, an alkyl amine renin inhibitor with potential for clinical utility.
Jia et al.
ACS Med.Chem.Lett., 2011;2:747
Renin inhibitor VTP-27999 differs from aliskiren: focus on their intracellular accumulation and the (pro)renin receptor.
Lu et al.
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