Molecular structure of IRL-2500, CAS Number: 169545-27-1
IRL-2500 (CAS 169545-27-1)
Alternate Names:
IRL-2500 is known as an ETB antagonist.
Application:
IRL-2500 is potent endothelin receptor antagonist that can inhibit ETB receptor-mediated blood pressure increase and renal vascular resistance.
CAS Number:
169545-27-1
Purity:
≥99%
Molecular Weight:
573.69
Molecular Formula:
C36H35N3O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
IRL-2500 is a potent, selective endothelin receptor antagonist. IRL-2500 displays selectivity for ETB receptors with an IC50 value of 1.3 for ETB receptors, and 94 nM for ETA receptors. In vivo, IRL-2500 was found to inhibit ETB receptor-mediated blood pressure increase in rats. Again in vivo, IRL-2500 was able to inhibit renal vascular resistance in rats in vivo.
IRL-2500 (CAS 169545-27-1) References
- Cytokines induce increased endothelin ET(B) receptor-mediated contraction. | Uddman, E., et al. 1999. Eur J Pharmacol. 376: 223-32. PMID: 10448880
- Effect of a novel bifunctional endothelin receptor antagonist, IRL 3630A, on guinea pig respiratory mechanics. | Makatani, M., et al. 2000. Eur J Pharmacol. 406: 139-47. PMID: 11011045
- Use of A-192621 and IRL-2500 to unmask the mesenteric and renal vasodilator role of endothelin ET(B) receptors. | Leung, SW., et al. 2002. J Cardiovasc Pharmacol. 39: 533-43. PMID: 11904527
- Intracrine endothelin signaling evokes IP3-dependent increases in nucleoplasmic Ca²⁺ in adult cardiac myocytes. | Merlen, C., et al. 2013. J Mol Cell Cardiol. 62: 189-202. PMID: 23756157
- Improvement of cold injury-induced mouse brain edema by endothelin ETB antagonists is accompanied by decreases in matrixmetalloproteinase 9 and vascular endothelial growth factor-A. | Michinaga, S., et al. 2015. Eur J Neurosci. 42: 2356-70. PMID: 26174228
- Design, Synthesis, and Biological Evaluation of Allosteric Effectors That Enhance CO Release from Carboxyhemoglobin. | Goldstein, SR., et al. 2018. ACS Med Chem Lett. 9: 714-718. PMID: 30034606
- Crystal structure of human endothelin ETB receptor in complex with peptide inverse agonist IRL2500. | Nagiri, C., et al. 2019. Commun Biol. 2: 236. PMID: 31263780
- Delineation of endothelin receptor subtypes in rat and rabbit aortas. | Shetty, SS., et al. 1995. J Cardiovasc Pharmacol. 26 Suppl 3: S310-3. PMID: 8587398
- Effects of the ETB-selective antagonist IRL 2500 in conscious spontaneously hypertensive and Wistar-Kyoto rats. | Webb, RL., et al. 1995. J Cardiovasc Pharmacol. 26 Suppl 3: S389-92. PMID: 8587423
- Characterization of a potent and selective endothelin-B receptor antagonist, IRL 2500. | Balwierczak, JL., et al. 1995. J Cardiovasc Pharmacol. 26 Suppl 3: S393-6. PMID: 8587424
- Endothelin evokes efflux of glutamate in cultures of rat astrocytes. | Sasaki, Y., et al. 1997. J Neurochem. 68: 2194-200. PMID: 9109548
- Regional variation in appearance of vascular contractile endothelin-B receptors following organ culture. | Adner, M., et al. 1998. Cardiovasc Res. 37: 254-62. PMID: 9539881
- Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity. | Sakaki, J., et al. 1998. Bioorg Med Chem Lett. 8: 2241-6. PMID: 9873521
Inhibitor of:
ETBR.Activator of:
Dear.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
IRL-2500, 10 mg | sc-204018 | 10 mg | $265.00 | |||
IRL-2500, 50 mg | sc-204018A | 50 mg | $1020.00 |