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VTP-27999 Hydrochloride


Cat No.
CEI-1575
Description
VTP-27999 Hydrochloride is a potent inhibitor of renin with IC50 value of 0.3 nM for human renin.
Product Overview
VTP-27999 hydrochlorideis a highly potent and selective renin inhibitor (IC50 = 0.47 nM). It exhibits >1000 selectivity for renin over >150 receptors, ion channels and enzymes. VTP-27999 hydrochloride is hydrochloride salt form of VTP-27999.Renin is an asparyl protease that cleaves angiotensinogen into angiotension I in the plasma. It functions as a regulator of blood pressure and sodium homeostasis. In vitro, VTP-27999 increases renin immunoreactivity by >30%, it bind to acid-activated, intact prorenin and promotes immunoreactivity in a renin assay. In vascular smooth muscle cells, VTP-27999 also blocks renins ability to activate extracellular signal-regulated kinase 1/2 phosphorylation. In double transgenic rats engineered to express human renin and angiotensinogen with severe hypertension, 24 h treatment of 10 mg/kg VTP-27999 induces a greater reduction in mean arterial blood pressure and a longer duration of action.
CAS No.
1264191-73-2
Molecular Weight
561.54
Purity
0.98
Storage
Store at -20°C
Synonyms
VTP27999 Hydrochloride; VTP 27999 Hydrochloride
Targets
human renin
IC50
0.3 nM
Molecular Formula
C26H42Cl2N4O5
Chemical Name
methyl N-[2-[(R)-(3-chlorophenyl)-[1-[[(2S)-2-(methylamino)-3-[(3R)-oxan-3-yl]propyl]carbamoyl]piperidin-3-yl]methoxy]ethyl]carbamate; hydrochloride
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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