IRL-2500

Modify Date: 2024-01-03 08:11:38

IRL-2500 Structure
IRL-2500 structure
Common Name IRL-2500
CAS Number 169545-27-1 Molecular Weight 573.68100
Density 1.246g/cm3 Boiling Point 893.7ºC at 760mmHg
Molecular Formula C36H35N3O4 Melting Point 83-88ºC
MSDS N/A Flash Point 494.3ºC

 Use of IRL-2500


IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo[1].

 Names

Name (2S)-2-[[(2R)-2-[(3,5-dimethylbenzoyl)-methylamino]-3-(4-phenylphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoic acid
Synonym More Synonyms

 IRL-2500 Biological Activity

Description IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo[1].
Related Catalog
Target

ETB:1.3 nM (IC50)

ETA:94 nM (IC50)

In Vivo IRL 2500 (intravenous injection;10 mg/kg) inhibits the initial transient decrease in mean arterial pressure (MAP) induced by the ETB-selective agonist IRL 1620 in rats, IRL 2500 also attenuates the IRL 1620-mediated increase in renal vascular resistance (RVR) in the anesthetized rat[1]. IRL 2500 (intravenous injection;10 mg/kg) pre-reatment significantly reduces the initial vasodepressor response to endothelin-1 (ET-1) and IRL 1620, however, it is not alters the secondary and sustained pressor response to these agonists[2].
References

[1]. Balwierczak JL, et al. Characterization of a potent and selective endothelin-B receptor antagonist, IRL 2500.J Cardiovasc Pharmacol. 1995;26 Suppl 3:S393-6.

[2]. Webb RL, et al. Effects of the ETB-selective antagonist IRL 2500 in conscious spontaneously hypertensive and Wistar-Kyoto rats.J Cardiovasc Pharmacol. 1995;26 Suppl 3:S389-92.

 Chemical & Physical Properties

Density 1.246g/cm3
Boiling Point 893.7ºC at 760mmHg
Melting Point 83-88ºC
Molecular Formula C36H35N3O4
Molecular Weight 573.68100
Flash Point 494.3ºC
Exact Mass 573.26300
PSA 102.50000
LogP 6.33800
Vapour Pressure 2.56E-34mmHg at 25°C
Index of Refraction 1.652
Storage condition 2-8°C

 Synonyms

Tocris-1838
IRL-2500