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Submit ReviewFR 139317
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)
Biological Activity for FR 139317
FR 139317 is 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 for FR 139317
| 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.
Product Datasheets for FR 139317
References for FR 139317
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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