Urotensin Receptor

Palosuran is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6??0.2 nM.

Urotensin II-related peptide is an analog of human urotensin II, exhibiting high affinity for the urotensin II receptor (UT). This peptide plays a significant role in cardiovascular regulation and may influence vascular smooth muscle contraction. It is commonly utilized in research focused on cardiovascular diseases, neurobiology, and the study of peptide receptor interactions.

SB-611812 is a selective antagonist of the urotensin II receptor (UTR), which plays a significant role in cardiovascular regulation. This compound is useful in investigating the pathological mechanisms underlying cardiovascular diseases and may aid in the development of novel therapeutic strategies targeting UTR-mediated pathways. Researchers can utilize SB-611812 to explore its effects on vascular function and cardiac remodeling in experimental models.

SB-706375 is an antagonist of the Urotensin II (UII) receptor, which plays a key role in renal physiology. By inhibiting this receptor, SB-706375 effectively decreases the kidney's response to UII and Urotensin-related peptide (URP), leading to a significant increase in Glomerular Filtration Rate (GFR). This compound is valuable for research applications focused on kidney diseases and hypertension, facilitating further understanding of renal function and associated pathologies.

GSK 1562590 hydrochloride is a potent and selective antagonist of the urotensin-II receptor (UT), exhibiting pKi values ranging from 9.14 to 9.66 across various mammalian species, including mouse, rat, cat, monkey, and human. This compound demonstrates significant inhibition of UT-mediated signaling pathways, making it valuable for research into cardiovascular and neuroendocrine disorders associated with urotensin-II. Its high affinity and selectivity position GSK 1562590 as an essential tool for studying the role of urotensin-II in physiological and pathological processes.

Urantide is a selective and competitive antagonist of the urotensin-II (UT) receptor, exhibiting a pKB of 8.3. This peptide effectively inhibits human urotensin-II (hU-II)-induced contractions in rat thoracic aorta ex vivo. Urantide is valuable for investigating the (patho)physiological roles of hU-II in the mammalian cardiovascular system, making it an important tool for related research applications.

Urotensin II (114-124), human, is a peptide comprising 11 amino acids that functions as a potent vasoconstrictor and an agonist for the urotensin receptor (GPR14). This compound is utilized in research to explore cardiovascular function and pathophysiology, particularly regarding its role in regulating vascular tone and blood pressure. Its biological activity makes it a valuable tool for studying urotensin signaling pathways and their implications in various disease states.

Palosuran hydrochloride is a selective, orally active antagonist of the urotensin II receptor, exhibiting an IC50 of 3.6 nM in CHO cell membranes expressing human recombinant receptors. This compound demonstrates potential to improve pancreatic and renal function in diabetic models, making it a valuable tool for research in metabolic and renal disorders. Its mechanism and target highlight its relevance in studies of urotensin II signaling pathways.

AC-7954 free base is a selective nonpeptidic agonist of the urotensin receptor, demonstrating an EC50 of 300 nM at the human urotensin II receptor. This compound is valuable for research focused on the urotensin signaling pathway and its implications in cardiovascular and metabolic disorders. Its specificity makes it suitable for studies investigating the physiological and pathological roles of urotensin receptors in various biological systems.

AC-7954 is a selective nonpeptidic agonist of the urotensin receptor, exhibiting an EC50 of 300 nM at the human urotensin II receptor. This compound plays a significant role in cardiovascular and metabolic research, with potential applications in the study of hypertension and heart failure. AC-7954 can be utilized to explore urotensin-related signaling pathways and their implications in various physiological processes.

SB-436811 is a selective antagonist of the urotensin-II receptor, exhibiting a pKi value of 6.7. This compound is primarily utilized in research focused on cardiovascular and metabolic disorders, where the urotensin-II pathway plays a significant role. By inhibiting urotensin-II activity, SB-436811 can aid in the exploration of its physiological effects and potential therapeutic applications.

Urotensin-II receptor antagonist-1 is a selective antagonist of the human Urotensin II receptor, exhibiting a Ki value of 16 nM in HEK293 cells expressing the recombinant receptor. This compound demonstrates significant biological activity by inhibiting cytochrome P450 enzymes, CYP2D6 and CYP3A4, with IC50 values of 0.75 μM and 1.4 μM, respectively. Additionally, it inhibits the κ-opioid receptor with an EC50 of 3.2 μM and targets cardiac sodium channels with a Ki of 2.5 μM. Research applications include studies of cardiovascular physiology and drug metabolism.