Chemical Structure : GSK1562590
CAS No.:
1003877-55-1
GSK1562590
(GSK-1562590)
Catalog No.: PC-28272Not For Human Use, Lab Use Only.
GSK1562590 is a potent, nonpeptidic antagonist of Urotensin II receptor (UT) with pKi of 9.14-9.66 for mammalian recombinant (mouse, rat, cat, monkey, human) and native (SJRH30 cells) UT.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
GSK1562590 is a potent, nonpeptidic antagonist of Urotensin II receptor (UT) with pKi of 9.14-9.66 for mammalian recombinant (mouse, rat, cat, monkey, human) and native (SJRH30 cells) UT.
GSK1562590 has >100-fold selectivity for UT versus 87 distinct mammalian GPCR, enzyme, ion channel and neurotransmitter uptake targets.
GSK1562590 is an insurmountable UT antagonist in rat, cat and hUT transgenic mouse arteries (pKb= 8.93–10.12 across species).
GSK1562590 inhibited the hU-II-induced systemic pressor response in anaesthetized cats.
GSK1562590 inhibited hU-II-induced contraction of rat aorta.
Physicochemical Properties
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M.Wt
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581.49
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Formula
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C30H30Cl2N4O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-4'-(1-(2-(6,7-dichloro-3-oxo-2,3-dihydro-4H-benzo[b][1,4]oxazin-4-yl)-N-methylacetamido)-2-(pyrrolidin-1-yl)ethyl)-[1,1'-biphenyl]-3-carboxamide
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References
1. Behm DJ, et al. Br J Pharmacol. 2010 Sep;161(1):207-28.
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