GJG057 | LTC4S inhibitor | Probechem Biochemicals

Chemical Structure : GJG057

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GJG057 (GJG-057)

货号: PC-23998Not For Human Use, Lab Use Only.

GJG057 is a potent, selective and orally bioavailable inhibitor of leukotriene C4 synthase (LTC4S) with IC50 of 44 nM in whole blood LTC4 release assay and 14 nM in enzymatic assays.

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生物&药学活性

GJG057 is a potent, selective and orally bioavailable inhibitor of leukotriene C4 synthase (LTC4S) with IC50 of 44 nM in whole blood LTC4 release assay and 14 nM in enzymatic assays.
GJG057 is over 40 times more potent than AZD9898.
GJG057 shows promising selectivity against a broad panel of receptors, enzymes, transporters, and channels with all IC50 values >10 μM.
GJG057 shows efficacy in a murine asthma exacerbation model as well as in a mastoparan-induced skin challenge PK/PD model.

物理化学性质&存储条件

分子量	456.42
分子式	C21H21F5N4O2
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	1-(3,4-Difluorophenyl)-9-(6-(2,2,2-trifluoroethoxy)pyrimidin-4-yl)-1,9-diazaspiro[5.5]undecan-2-one

参考文献

1. Thoma G, et al. J Med Chem. 2025 Feb 17. doi: 10.1021/acs.jmedchem.4c02897.

GJG057 (GJG-057)

生物&药学活性

物理化学性质&存储条件

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GJG057 (GJG-057)

生物&药学活性

物理化学性质&存储条件

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