VTP 27999 trifluoroacetate

Cat. No. 5563

VTP 27999 trifluoroacetate C26H41ClN4O5.CF3CO2H [1013937-63-7]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Lu et al (2014) Renin inhibitor VTP-27999 differs from aliskiren: focus on their intracellular accumulation and the (pro)renin receptor. J.Hypertens. 32 1255. PMID: 24637873.

Jia et al (2011) Discovery of VTP-27999, an alkyl amine renin inhibitor with potential for clinical utility. ACS Med.Chem.Lett. 2 747. PMID: 24900262.

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