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Submit ReviewVTP 27999 trifluoroacetate is a 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).
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 63.91 | 100 | |
DMSO | 63.91 | 100 |
The following data is based on the product molecular weight 639.1. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
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 |
References are publications that support the biological activity of the product.
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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