VTP-27999 Hydrochloride

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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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Project Description:

Our Products Cannot Be Used As Medicines Directly For Personal Use.

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