IRL-1620

Product Name:IRL-1620

CAS No:142569-99-1

Purity:95%

Molar Mass:1820.9

Chemical Formula:C86H117N17O27

Storage:Store at -20 degrees Celsius

Sequence:DEEAVYFAHLDIIW

Target:ETB

Application:

IRL-1620 is a synthetic peptide that acts as a highly selective agonist for the endothelin B (ETB) receptor. It is widely used in research to explore the role of the ETB receptor in various physiological processes, including vasodilation, neuroprotection, and blood flow regulation. IRL-1620 has shown potential in enhancing cerebral blood flow, making it of particular interest in studies related to stroke, neurodegenerative diseases, and other conditions where improved blood flow and neuroprotection are desired. This peptide is also utilized to investigate the therapeutic potential of ETB receptor activation in cardiovascular and renal diseases, as well as in cancer research due to its effects on tumor growth and metastasis.

Current Research:

IRL-1620 (also known as Sovateltide; CAS Number: 142569-99-1) is a synthetic, succinylated analog of endothelin-1, specifically designed as a highly selective agonist for the endothelin B (ET_B) receptor. Its amino acid sequence is: Suc-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp-OH In this sequence, the N-terminal aspartic acid is modified with a succinyl group, and glutamic acid residues at positions 9, and alanine residues at positions 11 and 15, are incorporated to enhance receptor selectivity. Pharmacological Profile: Receptor Selectivity: IRL-1620 exhibits a dissociation constant (K_i) of 16 pM for the ET_B receptor and 19 μM for the endothelin A (ET_A) receptor, indicating a selectivity ratio (K_i ETA/K_i ETB) of 120,000. This makes it 60 times more selective for the ET_B receptor compared to endothelin-3. Functional Activity: As an ET_B receptor agonist, IRL-1620 induces vasodilation by promoting the release of nitric oxide and prostacyclin from endothelial cells. It also facilitates the clearance of endothelin peptides from the circulation, contributing to vascular homeostasis. Research Applications: IRL-1620 is extensively utilized in both in vitro and in vivo studies to elucidate the physiological and pathological roles of ET_B receptors. Its applications include: Neuroprotection: In models of cerebral ischemia, IRL-1620 has demonstrated neuroprotective effects by enhancing angiogenesis and neurogenesis, thereby promoting neuronal function recovery. Cognitive Function: Administration of IRL-1620 has been shown to improve learning and memory in animal models, suggesting potential therapeutic applications in neurodegenerative diseases. Pain Management: Studies indicate that IRL-1620 can attenuate opioid tolerance without involving the nerve growth factor/phosphatidylinositol 3-kinase (NGF/PI3K) pathway, offering insights into pain management strategies. Handling and Storage: IRL-1620 is typically supplied as a lyophilized powder. For optimal stability, it should be stored desiccated at -20 degrees Celsius. Reconstitution can be performed using sterile distilled water or appropriate buffers, depending on experimental requirements. Safety Considerations: While specific safety data for IRL-1620 may be limited, standard laboratory precautions should be observed. This includes the use of personal protective equipment and proper laboratory ventilation to minimize exposure risks. In summary, IRL-1620 is a potent and selective ET_B receptor agonist that serves as a valuable tool in cardiovascular and neurological research, aiding in the understanding of endothelin-mediated physiological processes and their implications in health and disease.

Reference:

Briyal, S., Ranjan, A. K., Hornick, M. G., Puppala, A. K., Luu, T., & Gulati, A. (2019). Anti-apoptotic activity of ETB receptor agonist, IRL-1620, protects neural cells in rats with cerebral ischemia. Scientific reports, 9(1), 10439.