Cat. No. 1210
Chemical Name: N-[N-[N-[(Hexahydro-1H-azepin-1-yl)
Biological ActivityA 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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Palacios et al (2002) Role of endothelin ETA- and ETB-receptors in haemodynamic compensation following haemorrhage in anaesthetized rats. Br.J.Pharmacol. 135 876. PMID: 11861314.
Rubanyi and Polokoff (1994) Endothelins: molecular biology, biochemistry, pharmacology, physiology, and pathophysiology. Pharmacol.Rev. 46 325. PMID: 7831383.
Aramori et al (1993) Subtype selectivity of a novel endothelin antagonist, FR139317, for the two endothelin receptors in transfected Chinese hamster ovary cells. Mol.Pharmacol. 43 127. PMID: 8429819.
Sogabe et al (1993) Pharmacological profile of FR139317, a novel, potent endothelin ETA receptor antagonist. J.Pharmacol.Exp.Ther. 264 1040. PMID: 8450448.
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Keywords: FR 139317, supplier, potent, selective, ETA, antagonists, Receptors, ET, EndothelinA, FR139317, Tocris Bioscience, ETA Receptor Antagonist products