VTP-27999

VTP-27999 is a highly potent and selective renin inhibitor (IC50 = 0.47 nM). It exhibits >1000 selectivity for renin over >150 receptors, ion channels and enzymes. 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 renin's ability to activate extracellular signal-regulated kinase 1/2 phosphorylation. In double transgenic rats engineered to express human renin and angiotensinogen with severe hypertension, 24h treatment of 10 mg/kg VTP-27999 induces a greater reduction in mean arterial blood pressure and a longer duration of action.

Product information

CAS Number: 942142-51-0

Molecular Weight: 525.08

Formula: C26H41ClN4O5

Chemical Name: methyl N-{2-[(R)-(3-chlorophenyl)[(3R)-1-{[(2S)-2-(methylamino)-3-[(3R)-oxan-3-yl]propyl]carbamoyl}piperidin-3-yl]methoxy]ethyl}carbamate

Smiles: COC(=O)NCCO[C@H]([C@H]1CN(CCC1)C(=O)NC[C@H](C[C@H]1CCCOC1)NC)C1=CC(Cl)=CC=C1

InChiKey: NXWASIVXQMMPLM-ZXMXYHOLSA-N

InChi: InChI=1S/C26H41ClN4O5/c1-28-23(14-19-6-5-12-35-18-19)16-30-25(32)31-11-4-8-21(17-31)24(20-7-3-9-22(27)15-20)36-13-10-29-26(33)34-2/h3,7,9,15,19,21,23-24,28H,4-6,8,10-14,16-18H2,1-2H3,(H,29,33)(H,30,32)/t19-,21-,23+,24+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Krop M, Lu X, Verdonk K, Schalekamp MA et al. New renin inhibitor VTP-27999 alters renin immunoreactivity and does not unfold prorenin. Hypertension. 2013 May;61(5):1075-82.
2. Jia L, Simpson RD, Yuan J et al. Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility. ACS Med Chem Lett. 2011 Aug 9;2(10):747-51.

Products are for research use only. Not for human use.