R&D Systems Inc. Tocris Bioscience Boston Biochem

FR 139317

Cat. No. 1210

FR 139317 C33H44N6O5 [142375-60-8]

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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:
604.75
Formula:
C33H44N6O5
Solubility:
Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO
Purity:
>99 %
Storage:
Desiccate at +4°C
CAS No:
142375-60-8

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

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

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.

Rubanyi and Polokoff (1994) Endothelins: molecular biology, biochemistry, pharmacology, physiology, and pathophysiology. Pharmacol.Rev. 46 325. PMID: 7831383.

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.

If you know of a relevant citation for this product please let us know.

View Related Products by Target

Keywords: FR 139317, supplier, potent, selective, ETA, antagonists, Receptors, ET, EndothelinA, FR139317

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