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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)
Citations (1)

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
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
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.

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

Certificate of Analysis / Product Datasheet
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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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