Biological Activity
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. Behaves as a partial agonist in a calcium mobilization assay (in CHO cells expressing hUT receptors).
Technical Data
| M. Wt | 1075.26 |
| Formula | C51H66N10O12S2 |
| Sequence |
DXFWXYCV(Modifications: X-2 = Pen, X-5 = Orn, Trp-4 = D-Trp, Disulfide bridge: 2-7)
|
| Storage | Store at -20°C |
| CAS Number | 669089-53-6 |
| PubChem ID | 11520939 |
| InChI Key | VXLUBANOZQJZFE-QVKHRKAHSA-N |
| 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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 2 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1075.26. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.93 mL | 4.65 mL | 9.3 mL |
| 5 mM | 0.19 mL | 0.93 mL | 1.86 mL |
| 10 mM | 0.09 mL | 0.47 mL | 0.93 mL |
| 50 mM | 0.02 mL | 0.09 mL | 0.19 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Patacchini et al (2003) Urantide: an ultrapotent urotensin II antagonist peptide in the rat aorta. Br.J.Pharmacol. 140 1155 PMID: 14645137
Carotenuto et al (2014) Lead optimization of P5U and urantide: discovery of novel potent ligands at the urotensin-II receptor. J.Med.Chem. 57 5965 PMID: 24992374
Keywords: Urantide, supplier, Selective, competitive, urotensin, II, antagonists, [Pen5,DTrp7,Orn8]hU-II(4-11), Urotensin-II, Receptors, Urotensin-II, Receptors, Tocris Bioscience
