FR 139317 | Peptides (Cardiovascular) | Highly Potent, Selective ETA Antagonist | FR139317

Category:

Cat.No.	Product Name
1210	FR 139317

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FR 139317

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 ET_A endothelin receptor antagonist (K_i values are 1 nM and 7.3 μM at ET_A and ET_B subtypes respectively). Active in vivo.

Technical Data:

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

Resources:

Certificate of Analysis / MSDS:

Certificate of Analysis: View current batch

Product/Material Safety Data Sheet: View current batch

References:

Sogabe et al (1993) Pharmacological profile of FR139317, a novel, potent endothelin ET_A receptor antagonist. J.Pharmacol.Exp.Ther. 264 1040. 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. Rubanyi and Polokoff (1994) Endothelins: molecular biology, biochemistry, pharmacology, physiology, and pathophysiology. Pharmacol.Rev. 46 325. Palacios et al (2002) Role of endothelin ET_A- and ET_B-receptors in haemodynamic compensation following haemorrhage in anaesthetized rats. Br.J.Pharmacol. 135 876.

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Keywords: FR 139317, Peptides (Cardiovascular), Highly Potent, Selective ETA Antagonist, FR139317, Tocris Bioscience

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