169545-27-1

169545-27-1 structure

Name: IRL-2500
Chemical Name: (2S)-2-[[(2R)-2-[(3,5-dimethylbenzoyl)-methylamino]-3-(4-phenylphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoic acid
CAS Number: 169545-27-1
Molecular Formula: C₃₆H₃₅N₃O₄
Molecular Weight: 573.68100
Catalog: Signaling Pathways GPCR/G Protein Endothelin Receptor
Create Date: 2017-12-11 16:50:10
Modify Date: 2024-01-03 08:11:38
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].

Name	(2S)-2-[[(2R)-2-[(3,5-dimethylbenzoyl)-methylamino]-3-(4-phenylphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoic acid
Synonyms	Tocris-1838 IRL-2500

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	Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor
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.