Vipoglanstat (GS-248, BI 1029539) | mPGES-1 inhibitor

Chemical Structure : GS-248

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GS-248 (GS248, Vipoglanstat, BI 1029539)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	678.526
分子式	C30H34Cl2F5N5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

1. Malarvizhi Gurusamy, et al. J Transl Med. 2021 Aug 9;19(1):340.

GS-248 (GS248, Vipoglanstat, BI 1029539)

生物&药学活性

物理化学性质&存储条件

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GS-248 (GS248, Vipoglanstat, BI 1029539)

生物&药学活性

物理化学性质&存储条件

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