GLPBio

Urantide

Catalog No.: GC50138Purity:>98.00%
COASDSData Sheet
Urantide is a selective and competitive urotensin-II (UT) receptor antagonist, with the pKB value of 8.32.

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Urantide
Cas No.: 669089-53-6
1 mgIn Stock
$111.00
1
5 mgIn Stock
$226.00
1
10 mgIn Stock
$323.00
1
25 mgIn Stock
$529.00
1
50 mgIn Stock
$749.00
1
100 mgIn Stock
$987.00
1
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Beschreibung (Description)

Urantide is a selective and competitive urotensin-II (UT) receptor antagonist, with the pKB value of 8.32 [1]. Urantide can down-regulate the expression levels of UT and GPR14 in the liver and reduce the phosphorylation levels of Erk1/2 and JNK to prevent hepatic steatosis [2]. Urantide has been widely used to regulate the contraction and calcium release in the thoracic aorta of rats[3].

In vitro, Urantide (1μM) treatment for 48 hours significantly inhibited the urotensin II-stimulated proliferation of rat vascular smooth muscle cells (VSMCs) and induced cell cycle arrest[4]. Treatment with 1μM Urantide for 48 hours significantly reduced the expression of p-JAK2 and p-STAT3 proteins and the phenotypic transformation in rat VSMCs [5].

In vivo, Urantide treatment via intraperitoneal injection at a dose of 30μg/kg three times within 2 weeks significantly alleviated myocardial injury in rats with atherosclerosis[6]. Intraperitoneal injection of 10μg/kg/day dose of Urantide for 3 weeks significantly alleviated the increase in pulmonary arterial hypertension (PAH) induced by monocrotaline in rats and improved the structure and function of the right ventricle[7].

References:
[1] Carotenuto A, Auriemma L, Merlino F, et al. Lead optimization of P5U and urantide: discovery of novel potent ligands at the urotensin-II receptor[J]. Journal of Medicinal Chemistry, 2014, 57(14): 5965-5974.
[2] Cui H, Lin Y, Xie L, et al. Urantide decreases hepatic steatosis in rats with experimental atherosclerosis via the MAPK/Erk/JNK pathway[J]. Molecular Medicine Reports, 2021, 23(4): 1-10.
[3] Camarda V, Song W, Marzola E, et al. Urantide mimics urotensin-II induced calcium release in cells expressing recombinant UT receptors[J]. European journal of pharmacology, 2004, 498(1-3): 83-86.
[4] Zhao J, Zhang S F, Shi Y, et al. Effects of urotensin II and its specific receptor antagonist urantide on rat vascular smooth muscle cells[J]. Bosnian Journal of Basic Medical Sciences, 2013, 13(2): 78.
[5] Wang T, Xie L, Bi H, et al. Urantide alleviates the symptoms of atherosclerotic rats in vivo and in vitro models through the JAK2/STAT3 signaling pathway[J]. European Journal of Pharmacology, 2021, 902: 174037.
[6] Zhao J, Miao G, Wang T, et al. Urantide attenuates myocardial damage in atherosclerotic rats by regulating the MAPK signalling pathway[J]. Life sciences, 2020, 262: 118551.
[7] Wang Y, Tian W, Xiu C, et al. Urantide improves the structure and function of right ventricle as determined by echocardiography in monocrotaline-induced pulmonary hypertension rat model[J]. Clinical rheumatology, 2019, 38(1): 29-35.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

Rat vascular smooth muscle cells

Preparation Method

Rat vascular smooth muscle cells were grown in DMEM medium with 10% (v/v) fetal bovine serum (FBS), 100μg/ml streptomycin, and 100U/ml penicillin at 37°C in 5% CO2/atmosphere. Cells were seeded at a density of 1×105cells/ml in the 96-well plates and allowed to adhere in a 5% CO2 incubator at 37°C overnight. The cells were treated with different concentrations of Urantide (0, 0.001, 0.01, 0.1, and 1μM) in the presence of 0.01μM UT for 48h. Cell viability was evaluated.

Reaction Conditions

0, 0.001, 0.01, 0.1, and 1μM; 24h

Applications

Urantide treatment significantly reduced UT-induced cell proliferation of rat vascular smooth muscle cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

Wistar rats

Preparation Method

Wistar rats (3-month-old; 180-200g) were housed singly in a standard environment with food and water ad libitum. The rats were randomly assigned to one of the two groups: the early-treatment group (n=30) and the late-treatment group (n=30). Then, rats in each group were divided into three subgroups: control group, MCT group, and Urantide group (n=10 per subgroup). A PAH rat model was induced by the subcutaneous injection of 50mg/kg monocrotaline in the monocrotaline and Urantide groups. One week after PAH model construction, the surviving rats (some rats died of pulmonary edema or pulmonary hemorrhage within 1 week of monocrotaline injection) were injected intraperitoneally with either Urantide (10μg/kg/day) or an equal amount of normal saline (NS) (n=8) for 3 weeks. The normal control rats (n =10) received an equal volume of 0.9% saline for 3 weeks. Ultrasonic cardiogram was monitored at week 4.

Dosage form

10μg/kg/day for 3 weeks; i.p.

Applications

Urantide treatment significantly improved the structure and function of right ventricle in rats with PAH.

References:
[1] Zhao J, Zhang S F, Shi Y, et al. Effects of urotensin II and its specific receptor antagonist urantide on rat vascular smooth muscle cells[J]. Bosnian Journal of Basic Medical Sciences, 2013, 13(2): 78.
[2] Wang Y, Tian W, Xiu C, et al. Urantide improves the structure and function of right ventricle as determined by echocardiography in monocrotaline-induced pulmonary hypertension rat model[J]. Clinical rheumatology, 2019, 38(1): 29-35.

Produktdokumente (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
669089-53-6
SMILES
CC(C)[C@H](NC(=O)[C@@H]1CSSC(C)(C)[C@@H](NC(=O)[C@@H](N)CC(O)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(O)=O
Summenformel
C51H66N10O12S2
Molekulargewicht
1075.26
Löslichkeit
Soluble in DMSO
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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