Biological Activity
High affinity and selective urotensin II (UT) receptor antagonist (pKi values are 9.14, 9.28, 9.34, 9.64 and 9.66 at monkey, human, mouse, cat and rat recombinant receptors respectively). Exhibits selectivity for UT receptors over a range of GPCRs, ion channels, enzymes and neurotransmitter transporters. Supresses human urotensin-II (hU-II)-induced contraction of isolated rat aorta in vitro and ex vivo. Inhibits the hU-II-induced increase in mean blood pressure in vivo. Orally active.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Compound Libraries
GSK 1562590 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 617.95 |
| Formula | C30H30Cl2N4O4.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1003878-07-6 |
| PubChem ID | 46909864 |
| InChI Key | XTVXEMMIPYMBLL-SNYZSRNZSA-N |
| Smiles | NC(C1=CC=CC(C2=CC=[C@@]([C@@H](N(C(CN4C(C=C(Cl)C(Cl)=C5)=C5OCC4=O)=O)C)CN3CCCC3)C=C2)=C1)=O.Cl |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 61.8 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 617.95. 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 | 1.62 mL | 8.09 mL | 16.18 mL |
| 5 mM | 0.32 mL | 1.62 mL | 3.24 mL |
| 10 mM | 0.16 mL | 0.81 mL | 1.62 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Behm et al (2010) GSK1562590, a slowly dissociating urotensin-II receptor antagonist, exhibits prolonged pharmacodynamic activity ex vivo. Br.J.Pharmacol. 161 207 PMID: 20718751
Keywords: GSK 1562590 hydrochloride, supplier, GSK1562590, hydrochloride, high, affinity, selective, urotensin-II, receptors, antagonists, UT, hU-II, orally, active, peptides, Urotensin-II, Receptors, Urotensin-II, Receptors, Tocris Bioscience
