FR 139317

Pricing Availability   Qty
Cat.No. 1210 - FR 139317 | C33H44N6O5 | CAS No. 142375-60-8
Description: Highly potent, selective ETA antagonist
Chemical Name: N-[N-[N-[(Hexahydro-1H-azepin-1-yl)carbonyl]-L-leucyl]-1-methyl-D-tryptophyl]-3-(2-pyridinyl)-D-alanine
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

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.

Compound Libraries

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Technical Data

M. Wt 604.75
Formula C33H44N6O5
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 142375-60-8
PubChem ID 107810
InChI Key LIOKMIQQPDDTNO-UPRLRBBYSA-N
Smiles O=C([C@H](CC(C)C)NC(N1CCCCCC1)=O)N[C@@H]([C@@](N[C@H](CC2=NC=CC=C2)C(O)=O)=O)CC(C3=CC=CC=C34)=CN4C

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.

Solubility Data

Solubility Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO

References

References are publications that support the biological activity of the product.

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

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

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, FR 139317 supplier, potent, selective, ETA, antagonists, Receptors, ET, EndothelinA, FR139317, Endothelin, 1210, Tocris Bioscience

1 Citation for FR 139317

Citations are publications that use Tocris products. Selected citations for FR 139317 include:

Khodorova et al (2009) Early and late contributions of glutamate and CGRP to mechanical sensitization by endothelin-1. J Pain 10 740 PMID: 19559390


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.