Urotensin Receptor Antagonist

Palosuran (ACT-058362) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC₅₀ of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran can improves pancreatic and renal function in diabetic rats.

SB-611812 is a urotensin II receptor (UTR) antagonist with the potential in the research of cardiovascular disease.

SB-706375 is an antagonist of the Urotensin II (UII) receptor. By blocking the Urotensin II receptor, SB-706375 reduces the kidney's response to UII and Urotensin-related peptide (URP) and significantly increases the Glomerular Filtration Rate (GFR). SB-706375 can be used in research on kidney diseases and hypertension.

SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The K_i values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells.

GSK 1562590 hydrochloride is a high affinity and selective antagonist of urotensin-II receptor (UT), with pK_is of 9.14-9.66 for mammalian recombinant (mouse, rat, cat, monkey, human) and native UT.

Urantide is a selective and competitive urotensin-II (UT) receptor antagonist peptide (pKB=8.3) that blocks human urotensin-II (hU-II)-induced contractions in rat thoracic aorta ex vivo. Urantide can be used to study the (patho)physiological role of hU-II in the mammalian cardiovascular system.

Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC₅₀ of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran hydrochloride can improves pancreatic and renal function in diabetic rats.

SB-611812 (Standard) is the analytical standard of SB-611812. This product is intended for research and analytical applications. SB-611812 is a urotensin II receptor (UTR) antagonist with the potential in the research of cardiovascular disease.

Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, K_i=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC₅₀=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC₅₀=3.2 μM), targets cardiac sodium channels (K_i=2.5 μM).

[Orn5]-URP TFA is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC₅₀ of 7.24. [Orn5]-URP TFA displays no agonist activity.

UFP-803 is a potent urotensin-II receptor (UT) ligand. UFP-803 has lower residual agonist activity, so it may be an important tool for the investigations on the role played by the UT system in physiology and pathology.

[Orn5]-URP is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC₅₀ of 7.24. [Orn5]-URP displays no agonist activity.

UFP-803 TFA is a potent urotensin-II receptor (UT) ligand. UFP-803 TFA has lower residual agonist activity, so it may be an important tool for the investigations on the role played by the UT system in physiology and pathology.

SB-657510 (Standard) is the analytical standard of SB-657510 (HY-10656). This product is intended for research and analytical applications. SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The K_i values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells.

Palosuran (hydrochloride) (Standard) is the analytical standard of Palosuran (hydrochloride). This product is intended for research and analytical applications. Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran hydrochloride can improves pancreatic and renal function in diabetic rats.

SB-706375 (Standard) is the analytical standard of SB-706375 (HY-10657). This product is intended for research and analytical applications. SB-706375 is an antagonist of the Urotensin II (UII) receptor. By blocking the Urotensin II receptor, SB-706375 reduces the kidney's response to UII and Urotensin-related peptide (URP) and significantly increases the Glomerular Filtration Rate (GFR). SB-706375 can be used in research on kidney diseases and hypertension.

GSK-1440115 is an antagonist of the Urotensin II Receptor with an IC₅₀ value of 82.3 nM.

Palosuran (Standard) is the analytical standard of Palosuran. This product is intended for research and analytical applications. Palosuran (ACT-058362) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran can improves pancreatic and renal function in diabetic rats.

SB-436811 is a human urotensin-II receptor antagonist with a pK_i value of 6.7.