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Description: Potent ETB antagonist
Chemical Name: N-3-[1,1'-Biphenyl]-4-yl-N-(3,5-dimethylbenzoyl)-N-methyl-D-alanyl-L-tryptophan
Purity: ≥99% (HPLC)
Biological Activity for IRL-2500
IRL-2500 is a 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.
Compound Libraries for IRL-2500
IRL-2500 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for IRL-2500
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for IRL-2500
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. NaOH | 43.03 | 75 with gentle warming |
Preparing Stock Solutions for IRL-2500
The following data is based on the product molecular weight 573.69. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.75 mM | 2.32 mL | 11.62 mL | 23.24 mL |
| 3.75 mM | 0.46 mL | 2.32 mL | 4.65 mL |
| 7.5 mM | 0.23 mL | 1.16 mL | 2.32 mL |
| 37.5 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets for IRL-2500
References for IRL-2500
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for IRL-2500, please let us know.
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Keywords: IRL-2500, IRL-2500 supplier, Potent, ETB, antagonists, Receptors, Endothelin, IRL2500, 1838, Tocris Bioscience
1 Citation for IRL-2500
Citations are publications that use Tocris products. Selected citations for IRL-2500 include:
Merlen et al (2013) Intracrine endothelin signaling evokes IP3-dependent increases in nucleoplasmic Ca2+ in adult cardiac myocytes. J Mol Cell Cardiol 62 189 PMID: 23756157
Do you know of a great paper that uses IRL-2500 from Tocris? Please let us know.
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