GSK 1562590 hydrochloride

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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)
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Biological Activity for GSK 1562590 hydrochloride

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.

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 Data for GSK 1562590 hydrochloride

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 will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for GSK 1562590 hydrochloride

References for GSK 1562590 hydrochloride

References are publications that support the biological activity of the product.

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


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Citations for GSK 1562590 hydrochloride

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