Chemical Structure : VTP-27999 2,2,2-trifluoroacetate
CAS No.:
1013937-63-7
VTP-27999 2,2,2-trifluoroacetate
(VTP 27999, 2,2,2-trifluoroacetate;VTP27999, 2,2,2-trifluoroacetate;VTP-27999)
Catalog No. : PC-45865Not For Human Use, Lab Use Only.
A potent, highly selective renin inhibitor with IC50 of 0.47 nM.
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Purity & Documentation Purity:
>98% (HPLC) Select Batch: PC-4586501
Biological Activity
A potent, highly selective renin inhibitor with IC50 of 0.47 nM; displays >1000-fold selectivity for renin over a panel of >150 receptors, ion channels, and enzymes, and has an IC50 value >30 uM against CYP3A4; demonstrates >15% oral bioavailability in three species, oral efficacy in a double transgenic rat model of hypertension, and good exposure in humans.
Hypertension
Phase 1 Clinical
Physicochemical Properties
M.Wt
639.1039
Formula
C28H42ClF3N4O7
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
Carbamic acid, N-[2-[(R)-(3-chlorophenyl)[(3R)-1-[[[(2S)-2-(methylamino)-3-[(3R)-tetrahydro-2H-pyran-3-yl]propyl]amino]carbonyl]-3-piperidinyl]methoxy]ethyl]-, methyl ester, 2,2,2-trifluoroacetate (1:1)
References
1. Jia L, et al. ACS Med Chem Lett. 2011 Aug 9;2(10):747-51.
2. Krop M, et al. Hypertension. 2013 May;61(5):1075-82.
3. Balcarek J, et al. Hypertension. 2014 May;63(5):942-50.
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