Urantide |
Catalog No.GC50138
One-Click Copy Product Info
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Urantide is a selective and competitive urotensin-II (UT) receptor antagonist, with the pKB value of 8.32.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 669089-53-6
Sample solution is provided at 25 µL, 10mM.
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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.
| 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: | |
| Cas No. | 669089-53-6 | SDF | |
| Canonical 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 | ||
| Formula | C51H66N10O12S2 | M.Wt | 1075.26 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 930 μL | 4.65 mL | 9.3001 mL |
| 5 mM | 186 μL | 930 μL | 1.86 mL |
| 10 mM | 93 μL | 465 μL | 930 μL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)