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Category: 7TM ReceptorsarrowPeptides (Cardiovascular)arrowEndothelin ReceptorsarrowET-B Receptor Compounds
Cat.No. Product Name
1838 IRL-2500
Price and Availability

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IRL 2500
Chemical Name: N-3-[1,1'-Biphenyl]-4-yl-N-(3,5-dimethylbenzoyl)-N-meth yl-D-alanyl-L-tryptophan

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:

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M.Wt: 573.69
Formula: C36H35N3O4
Storage: Desiccate at RT
Solubility: Soluble to 100 mM in 1eq. NaOH
Purity: >99%
CAS No: [169545-27-1]

Resources:

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    References:

    Balwierczak et al (1995) Characterization of a potent and selective endothelin-B receptor antagonist, IRL 2500. J.Cardiovasc.Pharmacol. 26 S393. 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. 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.
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    Keywords: IRL 2500, Peptides (Cardiovascular), Potent ETB Antagonist, IRL2500, Tocris Bioscience

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