VTP 27999 trifluoroacetate

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Cat.No. 5563 - VTP 27999 trifluoroacetate | C26H41ClN4O5.CF3CO2H | CAS No. 1013937-63-7
Description: Highly potent and selective renin inhibitor
Chemical Name: Methyl N-[2-[(R)-(3-Chlorophenyl)[(3R)-1-[[[(2S)-2-(methylamino)-3-[(3R)-tetrahydro-2H-pyran-3-yl]propyl]amino]carbonyl]-3-piperidinyl]methoxy]ethyl]carbamate trifluoroacetate
Purity: ≥97% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Highly potent and selective renin inhibitor (IC50 = 0.47 nM). Displays >1000-fold selectivity over related and unrelated off-targets. Blocks renin-stimulated ERK1/2 phosphorylation in vascular smooth muscle cells. Exhibits a different mode of action to aliskiren (Cat. No. 5491).

Technical Data

M. Wt 639.1
Formula C26H41ClN4O5.CF3CO2H
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 1013937-63-7
PubChem ID 121513870
InChI Key SYWYSVAEGXHOJO-VIEYARBJSA-N
Smiles ClC1=CC=CC([C@H](OCCNC(OC)=O)[C@]2([H])CCCN(C(NC[C@@H](NC)C[C@H]3CCCOC3)=O)C2)=C1.OC(C(F)(F)F)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 63.91 100
water 63.91 100

Preparing Stock Solutions

The following data is based on the product molecular weight 639.1. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.56 mL 7.82 mL 15.65 mL
5 mM 0.31 mL 1.56 mL 3.13 mL
10 mM 0.16 mL 0.78 mL 1.56 mL
50 mM 0.03 mL 0.16 mL 0.31 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Jia et al (2011) Discovery of VTP-27999, an alkyl amine renin inhibitor with potential for clinical utility. ACS Med.Chem.Lett. 2 747 PMID: 24900262

Lu et al (2014) Renin inhibitor VTP-27999 differs from aliskiren: focus on their intracellular accumulation and the (pro)renin receptor. J.Hypertens. 32 1255 PMID: 24637873


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