Catalog Number: 1210
Chemical Name: N-[N-[N-[(Hexahydro-1H-azepin-1-yl)carbonyl]-L-leucyl]-1-methyl-D-tryptophyl]-3-(2-pyridinyl)-D-alanine
Biological Activity
A highly potent and selective ETA endothelin receptor antagonist (Ki values are 1 nM and 7.3 μM at ETA and ETB subtypes respectively). Active in vivo.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at +4°C
  • CAS No:
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.
Background References
  1. Subtype selectivity of a novel endothelin antagonist, FR139317, for the two endothelin receptors in transfected Chinese hamster ovary cells.
    Aramori et al.
    Mol.Pharmacol., 1993;43:127
  2. Role of endothelin ETA- and ETB-receptors in haemodynamic compensation following haemorrhage in anaesthetized rats.
    Palacios et al.
    Br.J.Pharmacol., 2002;135:876
  3. Endothelins: molecular biology, biochemistry, pharmacology, physiology, and pathophysiology.
    Rubanyi and Polokoff
    Pharmacol.Rev., 1994;46:325
  4. Pharmacological profile of FR139317, a novel, potent endothelin ETA receptor antagonist.
    Sogabe et al.
    J.Pharmacol.Exp.Ther., 1993;264:1040
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