urotensin-ii (ut)

[Orn5]-URP acetate is an effective and selective Urotensin-II receptor (UT) antagonist (pEC50 = 7.24). [Orn5]-URP exhibits no agonist activity.

SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models.

Urotensin-II receptor antagonist-1 (compound 1) is a human Urotensin II receptor antagonist with low oral bioavailability (F=0-3% in rats) and a Ki of 16 nM in HEK293 cells expressing human recombinant UT receptors. It inhibits cytochrome P450 enzymes (IC50=0.75 μM for CYP2D6; 1.4 μM for CYP3A4), suppresses κ opioid receptors (EC50=3.2 μM), and targets cardiac sodium channels (Ki=2.5 μM).

(±)-AC 7954 hydrochloride is a urotensin-II (UT) receptor activator.

urotensin II (UT) receptor antagonist

SB 611812 is an antagonist of urotensin-II (UT) and can be used in studies about the treatment of cardiovascular disease.

urotensin-II (UT) receptor antagonist

Urotensin II-related peptide, a human urotensin II analog, binds with high affinity to UT receptors.

Urotensin II-related peptide acetate are endogenous ligands of the orphan G-protein-coupled receptor GPR14, now known as UT. Urotensin II and URP exert a wide spectrum of biological effects on peripheral tissues including the cardiovascular system, airway smooth muscle, kidneys, and endocrine glands, while central administration elicits complex behavioral and cardiovascular responses, highlighting their physiological and pharmacological significance.

Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across isolated goby posterior intestine in 5% seawater-adapted solution.3In vivo, urotensin II (1.5-150 nmol/kg) decreases diastolic blood pressure and increases heart rate in anesthetized rats.4It also reduces the pressor responses to sympathetic nerve stimulation, norepinephrine , and vasopressin in pithed rats when administered at a dose of 150 nmol/kg. 1.Ames, R.S., Sarau, H.M., Chambers, J.K., et al.Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14Nature401(6750)282-286(1999) 2.Loretz, C.A., and Assad, J.A.Urotensin II lowers cytoplasmic free calcium concentration in goby enterocytes: Measurements using quin2Gen. Comp. Endocrinol.64(3)355-361(1986) 3.Loretz, C.A., Freel, R.W., and Bern, H.A.Specificity of response of intestinal ion transport systems to a pair of natural peptide hormone analogs: Somatostatin and urotensin IIGen. Comp. Endocrinol.52(2)198-206(1983) 4.Gibson, A., Wallace, P., and Bern, H.A.Cardiovascular effects of urotensin II in anesthetized and pithed ratsGen. Comp. Endocrinol.64(3)435-439(1986)

UFP-803 TFA, a potent ligand for the urotensin-II receptor (UT), exhibits minimal residual agonist activity, rendering it a valuable asset for exploring the UT system's function in physiology and pathology [1].

[Orn5]-URP TFA acts as a potent and selective antagonist exclusively targeting the Urotensin-II receptor (UT), devoid of any agonist activity, and demonstrates a significant inhibitory efficiency with a pEC50 value of 7.24 [1] [2].

Urotensin-II (UT) receptor pure antagonist (pEC50 = 7.24). Displays no agonist activity unlike other U-II/URP analogs. Inhibits the action of U-II in the rat aorta ring assay.

Urotensin-II (UT) receptor ligand; behaves as a silent antagonist in most in vitro assays and in vivo, but does retain small residual agonist activity under certain conditions in some assays. Competitively antagonizes U-II induced contractions in the rat

UFP 803 acetate is a potent ligand of urotensin-II (UT) receptor. UFP-803 displays the activity of a lower residual agonist.

Selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3). Blocks hU-II induced contractions in thoracic aorta ex vivo. Exhibits no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-induced relaxation. Behav

Urantide acetate is a selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3). Blocks hU-II induced contractions in thoracic aorta ex vivo. Exhibits no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-ind