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.
性状
Solid
IC50 & Target[1][2]
ETB
1.3 nM (IC50)
ETA
94 nM (IC50)
体内研究(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.
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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.