Biological Activity
Potent endothelin receptor antagonist; shows some selectivity for ETB receptors (IC50 values are 1.3 and 94 nM for ETB and ETA receptors respectively). Inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo.
Technical Data
| M. Wt | 573.69 |
| Formula | C36H35N3O4 |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 169545-27-1 |
| PubChem ID | 5311192 |
| InChI Key | UZDORQWMYRRLQV-JHOUSYSJSA-N |
| Smiles | O=C([C@@H](CC4=CC=C(C5=CC=CC=C5)C=C4)N(C)C(C3=CC(C)=CC(C)=C3)=O)N[C@H]([C@@](O)=O)CC1=CNC2=C1C=CC=C2 |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. NaOH | 43.03 | 75mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 573.69. 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 | 1.74 mL | 8.72 mL | 17.43 mL |
| 5 mM | 0.35 mL | 1.74 mL | 3.49 mL |
| 10 mM | 0.17 mL | 0.87 mL | 1.74 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.35 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Balwierczak et al (1995) Characterization of a potent and selective endothelin-B receptor antagonist, IRL 2500. J.Cardiovasc.Pharmacol. 26 S393 PMID: 8587424
Leung et al (2002) Use of A-192621 and IRL-2500 to unmask the mesenteric and renal vasodilator role of endothelin ETB receptors. J.Cardiovasc.Pharmacol. 39 533 PMID: 11904527
Webb et al (1995) Effects of the ETB-selective antagonist IRL 2500 in conscious spontaneously hypertensive and Wistar-Kyoto rats. J.Cardiovasc.Pharmacol. 26 S389 PMID: 8587423
Keywords: IRL-2500, supplier, Potent, ETB, antagonists, Receptors, Endothelin, IRL2500, Endothelin, ETB, Receptors, Endothelin, ETB, Receptors, Tocris Bioscience
