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GSK-588045

Chemical Structure : GSK-588045

CAS No.: 876922-98-4

GSK-588045 (GSK588045;GSK 588045)

Catalog No.: PC-61583Not For Human Use, Lab Use Only.

GSK-588045 is a potent and selective 5-HT1A/B/D receptor antagonist with Ki of 9.5/8.8/9.8, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GSK-588045 is a potent and selective 5-HT1A/B/D receptor antagonist with Ki of 9.5/8.8/9.8, respectively; exhibits high selectivity over human hERG potassium channels, favorable pharmacokinetics, and excellent activity in vivo in rodent pharmacodynamic (PD) models; demonstrates potential as a faster acting antidepressant/anxiolytic with reduced side-effect burden.

Anxiety

Phase 1 Clinical

Physicochemical Properties

M.Wt 468.561
Formula C27H28N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide

References

1. Bromidge SM, et al. J Med Chem. 2010 Aug 12;53(15):5827-43.

2. Comley RA, et al. Neuropharmacology. 2015 May;92:44-8.

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