IRL-2500
IRL-2500 Basic information
- Product Name:
- IRL-2500
- Synonyms:
-
- IRL-2500
- N-3-[1,1'-BIPHENYL]-4-YL-N-(3,5-DIMETHYLBENZOYL)-N-METHYL-D-ALANYL-L-TRYPTOPHAN
- L-Tryptophan, 3-[1,1'-biphenyl]-4-yl-N-(3,5-dimethylbenzoyl)-N-methyl-D-alanyl-
- ((R)-3-([1,1'-Biphenyl]-4-yl)-2-(N,3,5-trimethylbenzamido)propanoyl)-L-tryptophan
- IRL 2500, 10 mM in DMSO
- CAS:
- 169545-27-1
- MF:
- C36H35N3O4
- MW:
- 573.68
- Product Categories:
-
- Endothelin receptor
- Mol File:
- 169545-27-1.mol
IRL-2500 Chemical Properties
- Boiling point:
- 893.7±65.0 °C(Predicted)
- Density
- 1.246±0.06 g/cm3(Predicted)
- storage temp.
- Keep in dark place,Sealed in dry,Store in freezer, under -20°C
- solubility
- Soluble to 100 mM in 1eq. NaOH
- form
- Powder
- pka
- 3.34±0.10(Predicted)
- color
- White to light yellow
IRL-2500 Usage And Synthesis
Uses
IRL 2500 is a potent endothelin ETB selective antagonist.
Biological Activity
Potent endothelin receptor antagonist; shows some selectivity for ET B receptors (IC 50 values are 1.3 and 94 nM for ET B and ET A receptors respectively). Inhibits ET B receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo .
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].
IC 50
ETB: 1.3 nM (IC50); ETA: 94 nM (IC50)
storage
Desiccate at RT
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