urotensin

Palosuran (ACT-058362) (ACT-058362) is a new potent and specific antagonist of the human UT receptor.

Urotensin II, mouse acetate (9047-55-6 free base) is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.

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).

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

[Orn8]-Urotensin II is a Urotensin receptor ligand and a partial agonist at Urotensin receptors.

[Orn8]-Urotensin II acetate is a Urotensin receptor ligand and a partial agonist at Urotensin receptors.

Urotensin II, mouse acetate, serves as an endogenous ligand for the orphan G-protein-coupled receptor GPR14 or SENR and acts as a potent vasoconstrictor. Its physiological function extends to the central nervous system [1].

Urotensin I (Catostomus urotensin I) TFA is a CRF-like neuropeptide that acts as an agonist for CRF receptors, with pEC50 values of 11.46 for human CRF1, 9.36 for human CRF2, and 9.85 for rat CRF2α receptors in CHO cells. It shows binding affinities (Ki) of 0.4 nM for hCRF1, 1.8 nM for rCRF2α, and 5.7 nM for mCRF2β receptors [1] [2].

Urotensin I is, 41-aa neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectivel

Urotensin I acetate (83930-33-0 Free base) is a CRF-like neuropeptide (natural product), a CRF receptor agonist (EC50 as low as 3.5 pM for hCRF1, Ki=0.4 nM), with high affinity and receptor subtype selectivity, used for CRF receptor functional research.

Urotensin II (114-124), human TFA, is an 11-amino acid peptide with a potent vasoconstrictor effect and acts as an agonist for the orphan receptor GPR14.

Urotensin II (114-124), human, is an 11-amino acid residue peptide that acts as a potent vasoconstrictor and agonist for the orphan receptor GPR14.

Urotensin II (114-124), human acetate is an 11-amino acid residue peptide, is a potent vasoconstrictor and agonist for the orphan receptor GPR14.

Jump to search UTS2 Identifiers Aliases UTS2, PRO1068, U-II, UCN2, UII, urotensin 2 External IDs OMIM: 604097 MGI: 1346329 HomoloGene: 4939 GeneCards: UTS2 hide Gene location (Human) Chr. Chromosome 1 (human)[1] Band 1p36.23 Start 7,843,083 bp[1] En

Urotensin II, mouse TFA is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.

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)

FL104 is a potent agonist of small-molecule urotensin II receptor, pEC50= 7.11.

[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.

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

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

Palosuran hydrochloride 540769-28-6(free base)(ACT-058362 hydrochloride) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.

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