GSK 1562590 hydrochloride

Name: GSK 1562590 hydrochloride
Brand: Tocris Bioscience
SKU: 5110

Tocris Bioscience, part of Bio-Techne | Catalog # 5110

COA / SDS

High affinity, selective urotensin II (UT) receptor antagonist

Key Product Details

Description:	High affinity, selective urotensin II (UT) receptor antagonist
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
Purity:	≥98% (HPLC)
Molecular Weight:	617.95

View Full Technical Details for GSK 1562590 hydrochloride

Technical Data
Citations

Biological Activity for GSK 1562590 hydrochloride

GSK 1562590 hydrochloride is a high affinity and selective urotensin II (UT) receptor antagonist (pK_i 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.

Technical Data for GSK 1562590 hydrochloride

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GSK 1562590 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 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

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References for GSK 1562590 hydrochloride

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