FR 139317
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
FR 139317 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO |
Preparing Stock Solutions
The following data is based on the product molecular weight 604.75. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.65 mL | 8.27 mL | 16.54 mL |
| 5 mM | 0.33 mL | 1.65 mL | 3.31 mL |
| 10 mM | 0.17 mL | 0.83 mL | 1.65 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.33 mL |
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Product Datasheets
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
If you know of a relevant reference for FR 139317, please let us know.
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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
Do you know of a great paper that uses FR 139317 from Tocris? Please let us know.
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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 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.
