FR 139317
Tocris Bioscience, part of Bio-Techne | Catalog # 1210
Highly potent, selective ETA antagonist
Discontinued Product
1210 has been discontinued.
View all Endothelin ETA Receptor Antagonists products.
Key Product Details
Description
Highly potent, selective ETA antagonist
Product Description
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.Product Specifications
Molecular Weight
604.75
Formula
C33H44N6O5
Storage
Desiccate at +4°C
Purity
≥99% (HPLC)
Chemical Name
N-[N-[N-[(Hexahydro-1H-azepin-1-yl)carbonyl]-L-leucyl]-1-methyl-D-tryptophyl]-3-(2-pyridinyl)-D-alanine
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 100 | ||
| DMSO | 100 |
Preparing Stock Solutions
for FR 139317
The following data is based on the product molecular weight 604.75
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Sogabe Pharmacological profile of FR139317, a novel, potent endothelin ETA receptor antagonist. J.Pharmacol.Exp.Ther. 1993 PMID: 8450448
- Palacios Role of endothelin ETA- and ETB-receptors in haemodynamic compensation following haemorrhage in anaesthetized rats. Br.J.Pharmacol. 2002 PMID: 11861314
- Rubanyi and Polokoff Endothelins: molecular biology, biochemistry, pharmacology, physiology, and pathophysiology. Pharmacol.Rev. 1994 PMID: 7831383
- Aramori Subtype selectivity of a novel endothelin antagonist, FR139317, for the two endothelin receptors in transfected Chinese hamster ovary cells. Mol.Pharmacol. 1993 PMID: 8429819
Product Specific Notices for FR 139317
For research use only
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