FR 139317

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Cat.No. 1210 - FR 139317 | C33H44N6O5 | CAS No. 142375-60-8
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)
Datasheet
Citations
Literature

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

SolubilitySoluble 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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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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.

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Literature in this Area

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Pathways for FR 139317

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