VTP-27999 is a renin inhibitor (IC50 = 0.47 nM for the recombinant human enzyme).1 It is selective for renin over the aspartyl proteases β-secretase, cathepsin D, and cathepsin E at 10 ?M and is greater than 1,000-fold selective for renin over a panel of more than 250 receptors, ion channels, and enzymes. VTP-27999 (10 mg/kg, p.o.) reduces mean arterial pressure in rats expressing human renin and angiotensinogen, a double-transgenic model for angiotensin II-dependent hypertension.
1.Jia, L., Simpson, R.D., Yuan, J., et al.Discovery of VTP-27999, an alkyl amine renin inhibitor with potential for clinical utilityACS Med. Chem. Lett.2(10)747-751(2011)