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GS-248

Chemical Structure : GS-248

CAS No.: 1360622-01-0

GS-248 (GS248, Vipoglanstat, BI 1029539)

Catalog No.: PC-49465Not For Human Use, Lab Use Only.

Vipoglanstat (GS-248, BI 1029539) is a potent, selective and orally active membrane-associated prostaglandin E synthase-1 (mPGES-1) inhibitor with IC50 of 0.4 nM in human whole-blood assay (hWBA).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Vipoglanstat (GS-248, BI 1029539) is a potent, selective and orally active membrane-associated prostaglandin E synthase-1 (mPGES-1) inhibitor with IC50 of 0.4 nM in human whole-blood assay (hWBA).
GS-248 displays 1000-fold more potent than that of celecoxib.
GS-248 shows no cross reactivity with COX1 or COX2.
GS-248 displays IC50 values for human, dog, rat/mouse and minipig mPGES1 of 2.5, 1.3, > 1000 and 23 nM, respectively.
GS-248 shows significant activity comparable to celecoxib and indomethacin in mice.

Physicochemical Properties

M.Wt 678.526
Formula C30H34Cl2F5N5O3
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

2-((2,6-dichloro-3-(pivalamidomethyl)phenyl)amino)-6-(2,2-difluoroethoxy)-1-methyl-N-((1r,4r)-4-(trifluoromethyl)cyclohexyl)-1H-benzo[d]imidazole-5-carboxamide

References

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