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Results for "

urotensin receptor

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    34
    TargetMol | Inhibitors_Agonists
  • Peptide Products
    17
    TargetMol | Peptide_Products
Urotensin-II receptor antagonist-1
T2053471034708-07-0
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).
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10-14 weeks
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urotensin i acetate (83930-33-0 free base)
TP1199L
Urotensin I acetate, a CRF-like 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, respectively[1][2].
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TargetMol | Inhibitor Hot
FL104
FL-104, FL 104
T27328885672-81-1In house
FL104 is a potent agonist of small-molecule urotensin II receptor, pEC50= 7.11.
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6-8 weeks
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TargetMol | Inhibitor Sale
Urantide
TP2106669089-53-6
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
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4-6 weeks
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(±)-AC 7954 hydrochloride
T22476477313-09-0
(±)-AC 7954 hydrochloride is a urotensin-II (UT) receptor activator.
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6-8 weeks
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TargetMol | Inhibitor Sale
[Orn5]-URP acetate
[Orn5]-URP acetate(782485-03-4 free base)
TP1928L1
[Orn5]-URP acetate is an effective and selective Urotensin-II receptor (UT) antagonist (pEC50 = 7.24). [Orn5]-URP exhibits no agonist activity.
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TargetMol | Inhibitor Sale
Urotensin II, mouse acetate (9047-55-6 free base)
Urotensin II, mouse acetate
TP2165
Urotensin II, mouse acetate (9047-55-6 free base) is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.
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SB-657510
T12848474960-44-6
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.
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6-8 weeks
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Palosuran
ACT-058362
T2058540769-28-6
Palosuran (ACT-058362) (ACT-058362) is a new potent and specific antagonist of the human UT receptor.
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4-6 weeks
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GSK 1562590 hydrochloride
T228151003878-07-6
urotensin II (UT) receptor antagonist
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6-8 weeks
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SB 611812
T23323345892-71-9
SB 611812 is an antagonist of urotensin-II (UT) and can be used in studies about the treatment of cardiovascular disease.
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6-8 weeks
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SB 706375
T23326733734-61-7
urotensin-II (UT) receptor antagonist
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6-8 weeks
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AC-7954
T26542734528-95-1
AC-7954 is a potent and efficacious agonist of urotensin II receptor.
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6-8 weeks
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GSK 1440115
GSK1440115,GSK-1440115
T274411003878-16-7
GSK 1440115, an orally active urotensin II receptor antagonist, is used to treat asthma.
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8-10 weeks
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SB-436811
SB 436811
T28692346729-66-6
SB-436811 is an antagonist of human urotensin-II receptor.
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6-8 weeks
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Urolinin
nWWK-Tyr(3-NO2)-Abu
T29077
Urolinin is a linear peptidic Urotensin-II Receptor Agonist with low nanomolar potency as well as improved metabolic stability. Urolinin is a hexameric UIIR agonist with an EC50 of 4.75 nM and a metabolic stability of 1319 min, 6.3-fold higher than wild-t
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Urocortin III (human) (trifluoroacetate salt)
T35814
Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011). Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4 References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011).
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Urotensin II (goby) (trifluoroacetate salt)
T36729
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)
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[Orn8]-Urotensin II
[Orn8]-Urotensin II
T37527479065-85-5
[Orn8]-Urotensin II is a Urotensin receptor ligand and a partial agonist at Urotensin receptors.
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[Orn8]-Urotensin II acetate
T37527L
[Orn8]-Urotensin II acetate is a Urotensin receptor ligand and a partial agonist at Urotensin receptors.
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Palosuran hydrochloride 540769-28-6(free base)
ACT-058362 hydrochloride
T4689
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.
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GSK-1562590
T716421003877-55-1
GSK-1562590 is a urotensin-II receptor antagonist.
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6-8 weeks
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UFP-803 TFA
T75827
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].
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[Orn5]-URP TFA
T75828
[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].
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