Chemical Structure : VTP-27999
CAS No.:
942142-51-0
VTP-27999
(VTP27999;VTP 27999)
Catalog No. : PC-45864Not For Human Use, Lab Use Only.
A potent, highly selective renin inhibitor with IC50 of 0.47 nM.
Packing Price Stock Quantity 10 mg $528 In stock 0 1 2 3 4 5 50 mg $1100 In stock 0 1 2 3 4 5 100 mg $1760 In stock 0 1 2 3 4 5
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Purity & Documentation Purity:
>98% (HPLC) Select Batch: PC-4586401
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
525.0806
Formula
C26H41ClN4O5
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
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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