Catalog Number: 5563
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 Activity
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).
Technical Data
  • M.Wt:
    639.1
  • Formula:
    C26H41ClN4O5.CF3CO2H
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
    >97%
  • Storage:
    Store at -20°C
  • CAS No:
    1013937-63-7
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Discovery of VTP-27999, an alkyl amine renin inhibitor with potential for clinical utility.
    Jia et al.
    ACS Med. Chem. Lett., 2011;2:747
  2. Renin inhibitor VTP-27999 differs from aliskiren: focus on their intracellular accumulation and the (pro)renin receptor.
    Lu et al.
    J.Hypertens., 2014;32:1255

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