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GSK682753A

Chemical Structure : GSK682753A

CAS No.: 1334294-76-6

GSK682753A (GSK 682753A;GSK-682753A)

Catalog No.: PC-42332Not For Human Use, Lab Use Only.

GSK682753A (GSK 682753A, GSK-682753A) is a potent, selective EBI-2 (GPR183) inhibitor with IC50 of 53.6 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK682753A (GSK 682753A, GSK-682753A) is a potent, selective EBI-2 (GPR183) inhibitor with IC50 of 53.6 nM.
GSK682753A displays high selectivity over other constitutively active receptors, including GPR39, the ghrelin receptor, GPR17, MC1R, and ORF74.
GSK682753A does not affect the cell surface expression of EBI2 in HEK293 cells.
GSK682753A dose-dependently suppresses the inhibition of forskolin-stimulated cAMP accumulation mediated by EBI2 with IC50 of 10.9 nM, inhibits EBI2-mediated ERK phosphorylation with IC50 of 76 nM.
GSK682753A inhibits the antibody-induced proliferation of murine WT B cells.

Physicochemical Properties

M.Wt 479.78344
Formula C23H21Cl3N2O3
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

DMSO: ≥ 27 mg/mL

Chemical Name/SMILES

1-Oxa-3,8-diazaspiro[4.5]decan-2-one, 8-[(2E)-3-(4-chlorophenyl)-1-oxo-2-propen-1-yl]-3-[(3,4-dichlorophenyl)methyl]-

References

1. Benned-Jensen T, et al. J Biol Chem. 2011 Aug 19;286(33):29292-302.

2. Benned-Jensen T, et al. FEBS Open Bio. 2013 Feb 19;3:156-60.

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