IRL 2500

SKU: orb1707172

Description

IRL 2500 is a selective endothelin receptor antagonist, exhibiting potent activity against the ETA receptor (IC50 = 1.3 nM) with significantly lower affinity for the ETB receptor (IC50 = 94 nM). This small molecule is a valuable research tool for investigating the endothelin system in cardiovascular and pulmonary disease models, both in vitro and in vivo.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 169545-27-1
• MW: 573.68
• Purity: 99.36% (May vary between batches)
• Formula: C₃₆H₃₅N₃O₄
• SMILES: CN([C@H](Cc1ccc(cc1)-c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(O)=O)C(=O)c1cc(C)cc(C)c1
• Target: Endothelin Receptor
• Solubility: DMSO:93.6 mg/mL (163.16 mM)

Bioactivity

• Target IC50:
  ETB:1.3 nM|ETA:94 nM
• In Vivo:
  In the anesthetized rat, IRL 2500 (10 mg/kg; i.v.) decreases the IRL 1620-mediated enhances renal vascular resistance. IRL 2500 suppresses the initial transient reduction in mean arterial pressure induced by IRL 1620. IRL 2500 (10 mg/kg; i.v.) pre-treatment reduces the initial vasodepressor response to endothelin-1 and IRL 1620 without altering the secondary and sustained pressor response.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IRL2500, IRL-2500, IRL 2500, Endothelin B receptor, Endothelin A receptor, EndothelinReceptor, Endothelin Receptor, ETB, ETA

Compound Identifiers

PubChem CID

5311192