Product Name | IRL1038 |
Product Quantity | 0.2mg |
Catalog Number | LT12002 |
Molecular Weight | 1409.7 |
Formula | C68H92N14O15S2 |
Sequence | CVYFCHLDIIW |
Purity | >95% |
Product Description | Cys–Val–Tyr–Phe–Cys–His–Leu–Asp–Ile–Ile–Trp, CVYFCHLDIIW, With a disulfide bridge between Cys¹ and Cys⁵, forming a constrained ring structure. IRL 1038 is an antagonist of the ETB receptor that is responsible for the release of relaxing factor from the vascular endothelium. IRL-1038 acts as a selective ETB receptor antagonist: At 3 µM concentration, it inhibits ETB receptor–mediated contractions in guinea pig ileal and tracheal smooth muscle without exhibiting agonistic activity. Notably, it has no effect on ETA receptor–mediated contractions in rat aortic smooth muscle, indicating receptor subtype specificity. IRL-1038 serves as a valuable tool for investigating ETB receptor signaling and its role in vascular contractility and endothelial function. As an ETB antagonist, it opens avenues for therapies targeting conditions such as hypertension, vasoconstrictive disorders, or pulmonary hypertension, where modulation of ETB activity is therapeutically relevant. |
Scientific Background | IRL1038 is a synthetic research peptide in the IRL1038 endothelin-receptor research peptide category. IRL1038 is the cyclic endothelin-1-derived fragment [Cys11,Cys15]endothelin-1(11-21), historically used as an ETB-receptor antagonist in vascular and receptor-pharmacology studies. The original 1992 report identifying IRL1038 as an ETB-selective antagonist was later retracted; therefore this description relies on subsequent experimental studies that used IRL1038 pharmacologically rather than on the retracted discovery paper. |
Research Applications | - ETB receptor pharmacology
- endothelin-dependent vascular response studies
- receptor antagonist control experiments
- endothelin subtype comparison assays
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Experimental Notes | The exact supplied sequence and modification state should be used when interpreting published results. Activity reported for a parent peptide, labeled derivative, formulation, species variant, or related analog should not automatically be assigned to this construct. |
Selected References | - IRL1038 selectively inhibits ETB-mediated endothelin-dependent relaxation
- ETB-mediated basilar artery relaxation studied with IRL1038
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