GSK2973980A | DGAT1 inhibitor | Probechem Biochemicals

Chemical Structure : GSK2973980A

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GSK2973980A (GSK 2973980A)

货号: PC-62635Not For Human Use, Lab Use Only.

GSK2973980A is a potent and selective DGAT1 inhibitor with IC50 of 3 nM, exhibits >2,900-fold selectivity over human DGAT2, ACAT1 and ACAT2 (IC50>10 uM).

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生物&药学活性

GSK2973980A is a potent and selective DGAT1 inhibitor with IC50 of 3 nM, exhibits >2,900-fold selectivity over human DGAT2, ACAT1 and ACAT2 (IC50>10 uM).
GSK2973980A exhibits IC50 value of 77 nM in the cell-based C2C12 assay, also has excellent cardiac ion channel profile with IC50 of >10 uM in the hERG, Nav1.5 and Cav1.2。
GSK2973980A demonstrates excellent DMPK profiles and in vivo efficacy in a postprandial lipid excursion model in mice.

物理化学性质&存储条件

分子量	534.443
分子式	C25H19F5N4O4
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	(S)-2-(6-(5-(3-(3,4-difluorophenyl)ureido)pyrazin-2-yl)-1-oxo-2-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)acetic acid

参考文献

1. Cheung M, et al. ACS Med Chem Lett. 2018 Jan 16;9(2):103-108.

GSK2973980A (GSK 2973980A)

生物&药学活性

物理化学性质&存储条件

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GSK2973980A (GSK 2973980A)

生物&药学活性

物理化学性质&存储条件

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