| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
GPR14[1]
Urotensin II (114‑124) binds with high affinity to the UT receptor (also known as GPR14). UT is a class A GPCR that is widely expressed in the cardiovascular system, including blood vessels, heart, and kidney. Upon activation, UT couples primarily to Galphaq/11, leading to phospholipase C activation, IP3 production, and intracellular calcium mobilization. |
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| ln Vitro |
Human Urotensin II (U-II) exhibits a strong affinity for recombinant human GPR14, and this binding is functionally linked to the mobilization of calcium. In a HEK-293 cell line expressing human GPR14 (EC50 = 0:62±0.17 nM, n=6), human urotensin II causes concentration-dependent increases in intracellular calcium[1].
In vitro, human urotensin II (114‑124) potently constricts isolated human coronary and pulmonary arteries with an EC₅0 in the low nanomolar range (1‑10 nM). The contractile effect is endothelium‑independent. In calcium mobilization assays using HEK‑293 cells over‑expressing the human UT receptor, the peptide stimulates a rapid and transient increase in intracellular Ca2+ with an EC₅0 of approximately 0.1‑1 nM. |
| ln Vivo |
In anesthetized non-human primates, human urotensin II (U-II) significantly raises total peripheral resistance, a reaction linked to severe heart contractile dysfunction[1].
In anesthetized rats and non‑human primates, intravenous bolus injection of urotensin II (114‑124) (0.1‑10 nmol/kg) produces a biphasic cardiovascular response: a rapid, transient hypotension followed by a prolonged, dose‑dependent increase in systemic vascular resistance and hypertension. In humans, the peptide causes vasoconstriction in skin microvessels and increases forearm vascular resistance. The hypertensive effect is mediated via the UT receptor on vascular smooth muscle. |
| Enzyme Assay |
The radioligand binding assay uses membrane preparations from HEK‑293 cells stably expressing the human UT receptor (GPR14). Membranes (20‑50 ug protein) are incubated with [¹2⁵I]‑urotensin II (0.1 nM) and increasing concentrations of unlabeled urotensin II (114‑124) (0.001‑1000 nM) in 50 mM HEPES buffer (pH 7.4, containing 5 mM MgCl2, 1% BSA). After 60 minutes at 25degC, bound radioactivity is separated by filtration through GF/C filters and counted. The specific binding is defined by 1 uM urotensin II. Kᵢ values are typically 0.1‑1 nM.
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| Cell Assay |
HEK‑293 cells expressing UT are loaded with the calcium‑sensitive fluorescent dye Fluo‑4 AM (5 uM) for 30 minutes at 37degC. After washing, cells are transferred to a fluorescence plate reader (e.g., FlexStation 3). Urotensin II (114‑124) is added by the instrument at concentrations ranging from 0.01 nM to 1 uM. The fluorescence change (excitation 494 nm, emission 516 nm) is recorded in real time for 90‑120 seconds. The peak fluorescence (relative to baseline) is plotted against the log of peptide concentration to determine the EC₅0.
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| Animal Protocol |
Male Sprague‑Dawley rats (300‑400 g) are anesthetized with urethane (1.5 g/kg, i.p.). The carotid artery and jugular vein are cannulated for blood pressure monitoring and peptide administration, respectively. After a stabilization period, increasing doses of urotensin II (114‑124) (0.01‑10 nmol/kg) are administered intravenously as a bolus. Mean arterial pressure and heart rate are recorded continuously for 30 minutes after each dose. The dose producing a 50% increase in mean arterial pressure (ED₅0) is determined.
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| ADME/Pharmacokinetics |
Urotensin II (114‑124) is a peptide and is rapidly degraded by proteases in the circulation. The half‑life in human plasma is only 2‑5 minutes. The TFA salt does not alter the pharmacokinetic profile. The peptide does not cross the blood‑brain barrier. In preclinical studies, it is typically administered as an acute bolus injection because continuous infusion would be required to maintain stable plasma levels.
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| Toxicity/Toxicokinetics |
When administered acutely at low doses (<1 nmol/kg), the peptide is well‑tolerated. At high doses (≥10 nmol/kg) in rats, prolonged hypertension (>30 minutes) leads to reflex bradycardia and, in some animals, cardiac arrhythmias. Chronic elevation of urotensin II is associated with cardiovascular remodeling and fibrosis. The TFA counterion is not toxic at these concentrations.
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| References | |
| Additional Infomation |
Urotensin II (114‑124) is a research tool for studying the UT receptor in cardiovascular physiology and disease. The full‑length urotensin II preproprotein is processed to the biologically active 11‑mer, which is sufficient for full agonist activity. The peptide is not approved for human use. Increased expression of urotensin II and its receptor has been documented in hypertension, heart failure, and diabetes, making UT a potential therapeutic target.
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| Molecular Formula |
C66H86F3N13O20S2
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| Molecular Weight |
1502.59
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| Related CAS # |
Urotensin II (114-124), human;251293-28-4
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| Appearance |
Solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O :~100 mg/mL (~66.55 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (66.55 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6655 mL | 3.3276 mL | 6.6552 mL | |
| 5 mM | 0.1331 mL | 0.6655 mL | 1.3310 mL | |
| 10 mM | 0.0666 mL | 0.3328 mL | 0.6655 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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