[CAS NO. 169545-27-1] IRL 2500
PRODUCTS SPECIFICATIONS [169545-27-1]
DESCRIPTION [169545-27-1]
Overview
| MDL | MFCD00948945 |
|---|---|
| Molecular Weight | 573.68 |
| Molecular Formula | C36H35N3O4 |
| SMILES | O=C(O)[C@H](CC1=CNC2=CC=CC=C12)NC([C@@H](CC3=CC=C(C4=CC=CC=C4)C=C3)N(C(C5=CC(C)=CC(C)=C5)=O)C)=O |
Summary
IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC 50 values of 1.3 and 94 nM for ET B and ET A receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo [1] .
IC50 & Target
|
ET B 1.3 nM (IC 50 ) |
ET A 94 nM (IC 50 ) |
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL ( 174.31 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7431 mL | 8.7157 mL | 17.4313 mL |
| 5 mM | 0.3486 mL | 1.7431 mL | 3.4863 mL |
| 10 mM | 0.1743 mL | 0.8716 mL | 1.7431 mL |
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.
