IRL 2500

Product details

• 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.
• Purity: >97%
• Concentration: 0.1-10 µM.
• Form: Lyophilized powder.
• Solubility: Soluble in NaOH. Centrifuge all products before use (10000 x g 5 min).
• Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration of at least 0.1 mg/mL. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. It is recommended to prepare fresh solutions in working buffers just before use. Repeat freeze-thawing may result in loss of activity
• Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
• Target: ET-B receptor
• Source: Synthetic
• Activity: IRL 2500 is a potent antagonist of endothelin ET-B receptors, exhibiting selectivity for ET-B over ET-A receptors when inhibiting the binding of [125I]-Endothein-1 (IC50 of 1.3 nM and 94 nM, respectively). IRL 2500 attenuates the effects of ETB-selective agonists in vitro and in-vivo, such as saraphotoxin S6c-mediated dog saphenous vein contraction or IRL-1620-induced transient decrease in arterial pressure and increase in renal vascular resistance in rat1,2.

Scientific background

IRL 2500 is a synthetic compound that acts as a potent and selective antagonist of ET-B (endothelin B) receptor, a receptor that belongs to the G protein-coupled receptors (GPCR).IRL 2500 is more selective for human ET-B over ET-A receptor and can be used to delineate responses mediated by the ETB receptor1. IRL 2500 demonstrates IC50 values of 1.3 nM and 94 nM for human ETB and ETA receptor expressed in transfected Chinese hamster ovary cells respectively1.Several in vitro studies have shown that IRL 2500 can inhibit the sarafotoxin S6c-mediated contraction of the dog saphenous vein and the sarafotoxin S6c-induced relaxation of the preconstricted rabbit mesenteric artery. IRL 2500 also attenuates the IRL 1620-mediated increase in renal vascular resistance and decrease in arterial pressure in the anesthetized rat1,2.Endothelin receptors are widely distributed in vascular and nonvascular tissues. ET-B receptor has equally high affinity for all endothelin isopeptides3. ET-B receptors play an important role in regulating renal function and blood pressure and are expressed in sensory nerves. They are mainly present in medium- and large-sized cell bodies of human trigeminal ganglia4.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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