GSK 1562590 hydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 5110
High affinity, selective urotensin II (UT) receptor antagonist
Key Product Details
Description
High affinity, selective urotensin II (UT) receptor antagonist
Product Description
GSK 1562590 hydrochloride is a 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.Product Specifications
Molecular Weight
617.95
Formula
C30H30Cl2N4O4.HCl
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
N-[(1R)-1-[3'-(Aminocarbonyl)[1,1'-biphenyl]-4-yl]-2-(1-pyrrolidinyl)ethyl]-6,7-dichloro-2,3-dihydro-N-methyl-3-oxo-4H-1,4-benzoxazine-4-acetamide hydrochloride
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 61.8 | 100 |
Preparing Stock Solutions
for GSK 1562590 hydrochloride
The following data is based on the product molecular weight 617.95
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Behm GSK1562590, a slowly dissociating urotensin-II receptor antagonist, exhibits prolonged pharmacodynamic activity ex vivo. Br.J.Pharmacol. 2010 PMID: 20718751
Product Specific Notices for GSK 1562590 hydrochloride
For research use only
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