IRL-1038

Product Name:IRL-1038

CAS No:144602-02-8

Purity:95%

Molar Mass:1409.7

Chemical Formula:C68H92N14O15S2

Storage:Store at -20 degrees Celsius

Sequence:CVYFCHLDIIW

Target:ETB

Application:

IRL-1038 is a synthetic peptide and a selective antagonist of the endothelin B (ETB) receptor. It is used primarily in research to study the physiological and pathological roles of endothelin, particularly in the context of cardiovascular and renal systems. By selectively inhibiting ETB receptor activity, IRL-1038 helps researchers investigate the receptor's involvement in vasodilation, blood pressure regulation, and the pathophysiology of diseases such as hypertension, heart failure, and pulmonary arterial hypertension. Its specificity makes it a valuable tool for exploring the therapeutic potential of targeting the ETB receptor in various endothelin-related conditions.

Current Research:

IRL-1038 (CAS: 144602-02-8) is a synthetic peptide that functions as a selective antagonist of the endothelin B (ET_B) receptor. Its sequence is Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-Ile-Ile-Trp, featuring a disulfide bridge between the cysteine residues at positions 1 and 5, which stabilizes its structure. Pharmacological Profile: Receptor Selectivity: IRL-1038 exhibits high affinity for ET_B receptors, with a dissociation constant (K_i) ranging from 6 to 11 nM. It demonstrates significantly lower affinity for endothelin A (ET_A) receptors, with a K_i of approximately 0.4 to 0.7 μM. Functional Activity: As an ET_B receptor antagonist, IRL-1038 inhibits ET_B receptor-mediated responses, such as endothelium-dependent vascular relaxation induced by endothelins. It does not significantly affect ET_A receptor-mediated contractions, indicating its selectivity. Research Applications: IRL-1038 is utilized in cardiovascular research to investigate the specific roles of ET_B receptors in vascular function and related pathologies. By selectively blocking ET_B receptors, it aids in delineating the contributions of these receptors to endothelin-induced vascular responses and in exploring potential therapeutic targets for cardiovascular diseases. Handling and Storage: For laboratory use, IRL-1038 is typically supplied as a lyophilized powder. It is recommended to store the compound desiccated at -20 degrees Celsius to maintain its stability and bioactivity. Safety Considerations: Appropriate safety measures should be implemented when handling IRL-1038, including the use of personal protective equipment and proper laboratory ventilation, to minimize exposure risks. In summary, IRL-1038 is a potent and selective ET_B receptor antagonist extensively utilized in research to explore endothelin-mediated physiological processes and their implications in cardiovascular health and disease.

Reference:

Peng, H. J., Dai, D. Z., Ji, H., & Dai, Y. (2010). The separate roles of endothelin receptors participate in remodeling of matrix metalloproteinase and connexin 43 of cardiac fibroblasts in maladaptive response to isoproterenol. European Journal of Pharmacology, 634(1-3), 101-106.