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
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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.
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 products' biological activity.
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: potent selective ETA antagonists Receptors ET EndothelinA FR139317 Endothelin ETA Receptors
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? If so please let us know.
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