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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
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.
View Related Products by Target
View Related Products by Product Action
Keywords: FR 139317, FR 139317 supplier, potent, selective, ETA, antagonists, Receptors, ET, EndothelinA, FR139317, Endothelin, 1210, Tocris Bioscience
Citations for FR 139317
Citations are publications that use Tocris products.
Currently there are no citations for FR 139317. Do you know of a great paper that uses FR 139317 from Tocris? Please let us know.
Reviews for FR 139317
There are currently no reviews for this product. Be the first to review FR 139317 and earn rewards!
Have you used FR 139317?
Submit a review and receive an Amazon gift card.
$10US/$10CAN/€7/£6 gift card for a review without an image
$25US/$25CAN/€18/£15 gift card for a review with an image
*Offer only valid in the USA / Canada, UK and Europe
Submit a ReviewLiterature 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.
Cardiovascular Research Product Guide
A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:
- Hypertension
- Thrombosis and Hemostasis
- Atherosclerosis
- Myocardial Infarction
- Ischemia/Reperfusion Injury
- Arrhythmias
- Heart Failure
GPCR Product Listing
A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:
- Rhodopsin-like Receptors
- Secretin-like Receptors
- Glutamate Receptors
- Frizzled Receptors
- GPCR Signaling
Peptide Hormone Receptors Product Listing
A collection of over 200 products for peptide hormone receptors, the listing includes research tools for the study of:
- Anterior Pituitary Regulation
- Blood Pressure Regulation
- Feeding and Appetite Regulation
- Glucose Regulation
- Peptide Hormone Processing
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.
